1787-10   Fasudil, Monohydrochloride   品牌 Biovision

Fasudil, Monohydrochloride

货号: 1787-10      产品名称: Fasudil, Monohydrochloride   品牌: Biovision 规格: 10 mg 3周到货 生化实验

Fasudil, Monohydrochloride
A Rho kinase (ROCK) inhibitor
Product Overview
Product Name: Fasudil, Monohydrochloride
Alternate Name/Synonyms: 1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt; HA-1077, Monohydrochloride; AT-877
Description: A cell-permeable Ca²⁺ antagonist and vasodilator. Inhibits protein kinase A (Ki = 1.6 µM), protein kinase G (Ki = 1.6 µM), myosin light chain kinase (Ki = 36 µM) and Rho kinase (ROCK; IC₅₀ = 10.7 µM. Fasudil also mobilizes adult neural stem cells in vivo.
Peptide Sequence: N/A
Appearance: White to off-white solid
Formulation: Water (175 mg/ml) or DMSO (10 mg/ml)
CAS Number: 105628-07-7
Molecular Formula: C₁₄H₁₇N₃O₂S•HCl
Molecular Weight: 327.83
Purity: ≥99% by HPLC
Solubility:Water (175 mg/ml) or DMSO (10 mg/ml)
Storage Temp.: -20°C
Shipping Conditions: gel pack
Handling: Protect from air and moisture
SMILES: C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
InChi: InChI=1S/C14H17N3O2S.ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;/h1,3-5,7,11,15H,2,6,8-10H2;1H
InChi Key: LFVPBERIVUNMGV-UHFFFAOYSA-N
PubChem CID: 163751
MDL Number: MFCD00943198
USAGE: For Research Use Only! Not For Use in Humans.

-20°C

1787-50   Fasudil, Monohydrochloride   品牌 Biovision

Fasudil, Monohydrochloride

货号: 1787-50      产品名称: Fasudil, Monohydrochloride   品牌: Biovision 规格: 50 mg 3周到货 生化实验

Fasudil, Monohydrochloride
A Rho kinase (ROCK) inhibitor
Product Overview
Product Name: Fasudil, Monohydrochloride
Alternate Name/Synonyms: 1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt; HA-1077, Monohydrochloride; AT-877
Description: A cell-permeable Ca²⁺ antagonist and vasodilator. Inhibits protein kinase A (Ki = 1.6 µM), protein kinase G (Ki = 1.6 µM), myosin light chain kinase (Ki = 36 µM) and Rho kinase (ROCK; IC₅₀ = 10.7 µM. Fasudil also mobilizes adult neural stem cells in vivo.
Peptide Sequence: N/A
Appearance: White to off-white solid
Formulation: Water (175 mg/ml) or DMSO (10 mg/ml)
CAS Number: 105628-07-7
Molecular Formula: C₁₄H₁₇N₃O₂S•HCl
Molecular Weight: 327.83
Purity: ≥99% by HPLC
Solubility:Water (175 mg/ml) or DMSO (10 mg/ml)
Storage Temp.: -20°C
Shipping Conditions: gel pack
Handling: Protect from air and moisture
SMILES: C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
InChi: InChI=1S/C14H17N3O2S.ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;/h1,3-5,7,11,15H,2,6,8-10H2;1H
InChi Key: LFVPBERIVUNMGV-UHFFFAOYSA-N
PubChem CID: 163751
MDL Number: MFCD00943198
USAGE: For Research Use Only! Not For Use in Humans.

-20°C

F-4660-1 g   Fasudil, Monohydrochloride Salt   品牌 LC

Fasudil, Monohydrochloride Salt

货号: F-4660-1 g      产品名称: Fasudil, Monohydrochloride Salt   品牌: LC 规格: 1 g

F-4660 Fasudil, Monohydrochloride Salt, >99%
[HA-1077, Monohydrochloride Salt] [1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt] [Eril] [AT-877] [HA1077] [HA 1077]
M.W. 327.83
C14H17N3O2S•HCl
[105628-07-7]
 M.I. 12:  3980
 M.I. 14:  3942
Storage:  Store at or below -20 ºC.  Solubility:  Very soluble in water, up to about 200 mg/mL ; soluble in DMSO up to about 95 mg/mL; not soluble in ethanol; addition of an aqueous solution of this monohydrochloride salt into a buffer solution may significantly alter its solubility.  Disposal:  A
Nomenclature.  Two names have been widely used for this compound, "HA-1077" and "Fasudil", and these names have been variously and inconsistently applied to the free base (a form that LC Labs does not sell), the monohydrochloride salt and the dihydrochloride salt forms.  For many years LC Labs has sold the dihydrochloride salt under the name HA-1077, Dihydrochloride Salt, Cat. No. H-2330.  For historical reasons and for continuity, we have elected to continue using the HA-1077 name for our dihydrochloride salt product, even though we recently introduced the monohydrochloride salt form under the name Fasudil, Monohydrochloride Salt, Cat. No. F-4660, as described on this page.
The monohydrochloride salt is the form used to prepare formulations of this drug for clinical use.  Note that the solubility properties of the mono- and di-HCl salts are different.
Kinase inhibitor; has antivasospastic properties.
Asano, T., et al.  "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinases."  Br. J. Pharmacol. 98:  1091-1100 (1989).
Sasaki, Y. and Sasaki, Y.  "Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator."  Biochem. Biophys. Res. Commun. 171:  1182-1187 (1990).
Seto, M., et al.  "Effects of HA 1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle."  Eur. J. Pharmacol. 195:  267-272 (1991).
Shibuya, O., et al.  The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:  53 (1988).
Shirotani, M. et al.  "A new type of vasodilator, HA 1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture."  J. Pharmacol. Exp. Ther. 259:  738-744 (1991).
Swärd, K. et al.  "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum."  J. Physiol. 522:  33-49 (2000).
Davies, S.P. et al.  "Specificity and mechanism of action of some commonly used protein kinase inhibitors."  Biochem. J. 351:  95-105 (2000).
This monohydrochloride salt form is the active ingredient in drug formulations marketed in Japan to treat cerebral vasospasm following surgery for subarachnoid hemorrhage and associated cerebral ischemic symptoms.  Zhao, J. et al.  "Effect of Fasudil Hydrochloride, a Protein Kinase Inhibitor, on Cerebral Vasospasm and Delayed Cerebral Ischemic Symptoms After Aneurysmal Subarachnoid Hemorrhage."  Neurologia Medico-Chirurgica 46:  421-428 (2006).  Also, the monohydrochloride form has been or presently is in human clinical trials for treatment of acute cerebral thrombosis, subarachnoid hemorrhage, and angina pectoris.
Related CAS numbers:  103745-39-7 for fasudil free base and 203911-27-7 for HA-1077 dihydrochloride salt.
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

 

 

 

-20 ºC

F-4660-10 g   Fasudil, Monohydrochloride Salt   品牌 LC

Fasudil, Monohydrochloride Salt

货号: F-4660-10 g      产品名称: Fasudil, Monohydrochloride Salt   品牌: LC 规格: 10 g

F-4660 Fasudil, Monohydrochloride Salt, >99%
[HA-1077, Monohydrochloride Salt] [1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt] [Eril] [AT-877] [HA1077] [HA 1077]
M.W. 327.83
C14H17N3O2S•HCl
[105628-07-7]
 M.I. 12:  3980
 M.I. 14:  3942
Storage:  Store at or below -20 ºC.  Solubility:  Very soluble in water, up to about 200 mg/mL ; soluble in DMSO up to about 95 mg/mL; not soluble in ethanol; addition of an aqueous solution of this monohydrochloride salt into a buffer solution may significantly alter its solubility.  Disposal:  A
Nomenclature.  Two names have been widely used for this compound, "HA-1077" and "Fasudil", and these names have been variously and inconsistently applied to the free base (a form that LC Labs does not sell), the monohydrochloride salt and the dihydrochloride salt forms.  For many years LC Labs has sold the dihydrochloride salt under the name HA-1077, Dihydrochloride Salt, Cat. No. H-2330.  For historical reasons and for continuity, we have elected to continue using the HA-1077 name for our dihydrochloride salt product, even though we recently introduced the monohydrochloride salt form under the name Fasudil, Monohydrochloride Salt, Cat. No. F-4660, as described on this page.
The monohydrochloride salt is the form used to prepare formulations of this drug for clinical use.  Note that the solubility properties of the mono- and di-HCl salts are different.
Kinase inhibitor; has antivasospastic properties.
Asano, T., et al.  "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinases."  Br. J. Pharmacol. 98:  1091-1100 (1989).
Sasaki, Y. and Sasaki, Y.  "Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator."  Biochem. Biophys. Res. Commun. 171:  1182-1187 (1990).
Seto, M., et al.  "Effects of HA 1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle."  Eur. J. Pharmacol. 195:  267-272 (1991).
Shibuya, O., et al.  The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:  53 (1988).
Shirotani, M. et al.  "A new type of vasodilator, HA 1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture."  J. Pharmacol. Exp. Ther. 259:  738-744 (1991).
Swärd, K. et al.  "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum."  J. Physiol. 522:  33-49 (2000).
Davies, S.P. et al.  "Specificity and mechanism of action of some commonly used protein kinase inhibitors."  Biochem. J. 351:  95-105 (2000).
This monohydrochloride salt form is the active ingredient in drug formulations marketed in Japan to treat cerebral vasospasm following surgery for subarachnoid hemorrhage and associated cerebral ischemic symptoms.  Zhao, J. et al.  "Effect of Fasudil Hydrochloride, a Protein Kinase Inhibitor, on Cerebral Vasospasm and Delayed Cerebral Ischemic Symptoms After Aneurysmal Subarachnoid Hemorrhage."  Neurologia Medico-Chirurgica 46:  421-428 (2006).  Also, the monohydrochloride form has been or presently is in human clinical trials for treatment of acute cerebral thrombosis, subarachnoid hemorrhage, and angina pectoris.
Related CAS numbers:  103745-39-7 for fasudil free base and 203911-27-7 for HA-1077 dihydrochloride salt.
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

 

 

 

-20 ºC

F-4660-2 g   Fasudil, Monohydrochloride Salt   品牌 LC

Fasudil, Monohydrochloride Salt

货号: F-4660-2 g      产品名称: Fasudil, Monohydrochloride Salt   品牌: LC 规格: 2 g

F-4660 Fasudil, Monohydrochloride Salt, >99%
[HA-1077, Monohydrochloride Salt] [1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt] [Eril] [AT-877] [HA1077] [HA 1077]
M.W. 327.83
C14H17N3O2S•HCl
[105628-07-7]
 M.I. 12:  3980
 M.I. 14:  3942
Storage:  Store at or below -20 ºC.  Solubility:  Very soluble in water, up to about 200 mg/mL ; soluble in DMSO up to about 95 mg/mL; not soluble in ethanol; addition of an aqueous solution of this monohydrochloride salt into a buffer solution may significantly alter its solubility.  Disposal:  A
Nomenclature.  Two names have been widely used for this compound, "HA-1077" and "Fasudil", and these names have been variously and inconsistently applied to the free base (a form that LC Labs does not sell), the monohydrochloride salt and the dihydrochloride salt forms.  For many years LC Labs has sold the dihydrochloride salt under the name HA-1077, Dihydrochloride Salt, Cat. No. H-2330.  For historical reasons and for continuity, we have elected to continue using the HA-1077 name for our dihydrochloride salt product, even though we recently introduced the monohydrochloride salt form under the name Fasudil, Monohydrochloride Salt, Cat. No. F-4660, as described on this page.
The monohydrochloride salt is the form used to prepare formulations of this drug for clinical use.  Note that the solubility properties of the mono- and di-HCl salts are different.
Kinase inhibitor; has antivasospastic properties.
Asano, T., et al.  "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinases."  Br. J. Pharmacol. 98:  1091-1100 (1989).
Sasaki, Y. and Sasaki, Y.  "Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator."  Biochem. Biophys. Res. Commun. 171:  1182-1187 (1990).
Seto, M., et al.  "Effects of HA 1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle."  Eur. J. Pharmacol. 195:  267-272 (1991).
Shibuya, O., et al.  The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:  53 (1988).
Shirotani, M. et al.  "A new type of vasodilator, HA 1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture."  J. Pharmacol. Exp. Ther. 259:  738-744 (1991).
Swärd, K. et al.  "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum."  J. Physiol. 522:  33-49 (2000).
Davies, S.P. et al.  "Specificity and mechanism of action of some commonly used protein kinase inhibitors."  Biochem. J. 351:  95-105 (2000).
This monohydrochloride salt form is the active ingredient in drug formulations marketed in Japan to treat cerebral vasospasm following surgery for subarachnoid hemorrhage and associated cerebral ischemic symptoms.  Zhao, J. et al.  "Effect of Fasudil Hydrochloride, a Protein Kinase Inhibitor, on Cerebral Vasospasm and Delayed Cerebral Ischemic Symptoms After Aneurysmal Subarachnoid Hemorrhage."  Neurologia Medico-Chirurgica 46:  421-428 (2006).  Also, the monohydrochloride form has been or presently is in human clinical trials for treatment of acute cerebral thrombosis, subarachnoid hemorrhage, and angina pectoris.
Related CAS numbers:  103745-39-7 for fasudil free base and 203911-27-7 for HA-1077 dihydrochloride salt.
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

 

 

 

-20 ºC

F-4660-250 mg   Fasudil, Monohydrochloride Salt   品牌 LC

Fasudil, Monohydrochloride Salt

货号: F-4660-250 mg      产品名称: Fasudil, Monohydrochloride Salt   品牌: LC 规格: 250 mg

F-4660 Fasudil, Monohydrochloride Salt, >99%
[HA-1077, Monohydrochloride Salt] [1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt] [Eril] [AT-877] [HA1077] [HA 1077]
M.W. 327.83
C14H17N3O2S•HCl
[105628-07-7]
 M.I. 12:  3980
 M.I. 14:  3942
Storage:  Store at or below -20 ºC.  Solubility:  Very soluble in water, up to about 200 mg/mL ; soluble in DMSO up to about 95 mg/mL; not soluble in ethanol; addition of an aqueous solution of this monohydrochloride salt into a buffer solution may significantly alter its solubility.  Disposal:  A
Nomenclature.  Two names have been widely used for this compound, "HA-1077" and "Fasudil", and these names have been variously and inconsistently applied to the free base (a form that LC Labs does not sell), the monohydrochloride salt and the dihydrochloride salt forms.  For many years LC Labs has sold the dihydrochloride salt under the name HA-1077, Dihydrochloride Salt, Cat. No. H-2330.  For historical reasons and for continuity, we have elected to continue using the HA-1077 name for our dihydrochloride salt product, even though we recently introduced the monohydrochloride salt form under the name Fasudil, Monohydrochloride Salt, Cat. No. F-4660, as described on this page.
The monohydrochloride salt is the form used to prepare formulations of this drug for clinical use.  Note that the solubility properties of the mono- and di-HCl salts are different.
Kinase inhibitor; has antivasospastic properties.
Asano, T., et al.  "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinases."  Br. J. Pharmacol. 98:  1091-1100 (1989).
Sasaki, Y. and Sasaki, Y.  "Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator."  Biochem. Biophys. Res. Commun. 171:  1182-1187 (1990).
Seto, M., et al.  "Effects of HA 1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle."  Eur. J. Pharmacol. 195:  267-272 (1991).
Shibuya, O., et al.  The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:  53 (1988).
Shirotani, M. et al.  "A new type of vasodilator, HA 1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture."  J. Pharmacol. Exp. Ther. 259:  738-744 (1991).
Swärd, K. et al.  "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum."  J. Physiol. 522:  33-49 (2000).
Davies, S.P. et al.  "Specificity and mechanism of action of some commonly used protein kinase inhibitors."  Biochem. J. 351:  95-105 (2000).
This monohydrochloride salt form is the active ingredient in drug formulations marketed in Japan to treat cerebral vasospasm following surgery for subarachnoid hemorrhage and associated cerebral ischemic symptoms.  Zhao, J. et al.  "Effect of Fasudil Hydrochloride, a Protein Kinase Inhibitor, on Cerebral Vasospasm and Delayed Cerebral Ischemic Symptoms After Aneurysmal Subarachnoid Hemorrhage."  Neurologia Medico-Chirurgica 46:  421-428 (2006).  Also, the monohydrochloride form has been or presently is in human clinical trials for treatment of acute cerebral thrombosis, subarachnoid hemorrhage, and angina pectoris.
Related CAS numbers:  103745-39-7 for fasudil free base and 203911-27-7 for HA-1077 dihydrochloride salt.
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

 

 

 

-20 ºC

F-4660-5 g   Fasudil, Monohydrochloride Salt   品牌 LC

Fasudil, Monohydrochloride Salt

货号: F-4660-5 g      产品名称: Fasudil, Monohydrochloride Salt   品牌: LC 规格: 5 g

F-4660 Fasudil, Monohydrochloride Salt, >99%
[HA-1077, Monohydrochloride Salt] [1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt] [Eril] [AT-877] [HA1077] [HA 1077]
M.W. 327.83
C14H17N3O2S•HCl
[105628-07-7]
 M.I. 12:  3980
 M.I. 14:  3942
Storage:  Store at or below -20 ºC.  Solubility:  Very soluble in water, up to about 200 mg/mL ; soluble in DMSO up to about 95 mg/mL; not soluble in ethanol; addition of an aqueous solution of this monohydrochloride salt into a buffer solution may significantly alter its solubility.  Disposal:  A
Nomenclature.  Two names have been widely used for this compound, "HA-1077" and "Fasudil", and these names have been variously and inconsistently applied to the free base (a form that LC Labs does not sell), the monohydrochloride salt and the dihydrochloride salt forms.  For many years LC Labs has sold the dihydrochloride salt under the name HA-1077, Dihydrochloride Salt, Cat. No. H-2330.  For historical reasons and for continuity, we have elected to continue using the HA-1077 name for our dihydrochloride salt product, even though we recently introduced the monohydrochloride salt form under the name Fasudil, Monohydrochloride Salt, Cat. No. F-4660, as described on this page.
The monohydrochloride salt is the form used to prepare formulations of this drug for clinical use.  Note that the solubility properties of the mono- and di-HCl salts are different.
Kinase inhibitor; has antivasospastic properties.
Asano, T., et al.  "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinases."  Br. J. Pharmacol. 98:  1091-1100 (1989).
Sasaki, Y. and Sasaki, Y.  "Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator."  Biochem. Biophys. Res. Commun. 171:  1182-1187 (1990).
Seto, M., et al.  "Effects of HA 1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle."  Eur. J. Pharmacol. 195:  267-272 (1991).
Shibuya, O., et al.  The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:  53 (1988).
Shirotani, M. et al.  "A new type of vasodilator, HA 1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture."  J. Pharmacol. Exp. Ther. 259:  738-744 (1991).
Swärd, K. et al.  "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum."  J. Physiol. 522:  33-49 (2000).
Davies, S.P. et al.  "Specificity and mechanism of action of some commonly used protein kinase inhibitors."  Biochem. J. 351:  95-105 (2000).
This monohydrochloride salt form is the active ingredient in drug formulations marketed in Japan to treat cerebral vasospasm following surgery for subarachnoid hemorrhage and associated cerebral ischemic symptoms.  Zhao, J. et al.  "Effect of Fasudil Hydrochloride, a Protein Kinase Inhibitor, on Cerebral Vasospasm and Delayed Cerebral Ischemic Symptoms After Aneurysmal Subarachnoid Hemorrhage."  Neurologia Medico-Chirurgica 46:  421-428 (2006).  Also, the monohydrochloride form has been or presently is in human clinical trials for treatment of acute cerebral thrombosis, subarachnoid hemorrhage, and angina pectoris.
Related CAS numbers:  103745-39-7 for fasudil free base and 203911-27-7 for HA-1077 dihydrochloride salt.
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

 

 

 

-20 ºC.

F-4660-500 mg   Fasudil, Monohydrochloride Salt   品牌 LC

Fasudil, Monohydrochloride Salt

货号: F-4660-500 mg      产品名称: Fasudil, Monohydrochloride Salt   品牌: LC 规格: 500 mg

F-4660 Fasudil, Monohydrochloride Salt, >99%
[HA-1077, Monohydrochloride Salt] [1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt] [Eril] [AT-877] [HA1077] [HA 1077]
M.W. 327.83
C14H17N3O2S•HCl
[105628-07-7]
 M.I. 12:  3980
 M.I. 14:  3942
Storage:  Store at or below -20 ºC.  Solubility:  Very soluble in water, up to about 200 mg/mL ; soluble in DMSO up to about 95 mg/mL; not soluble in ethanol; addition of an aqueous solution of this monohydrochloride salt into a buffer solution may significantly alter its solubility.  Disposal:  A
Nomenclature.  Two names have been widely used for this compound, "HA-1077" and "Fasudil", and these names have been variously and inconsistently applied to the free base (a form that LC Labs does not sell), the monohydrochloride salt and the dihydrochloride salt forms.  For many years LC Labs has sold the dihydrochloride salt under the name HA-1077, Dihydrochloride Salt, Cat. No. H-2330.  For historical reasons and for continuity, we have elected to continue using the HA-1077 name for our dihydrochloride salt product, even though we recently introduced the monohydrochloride salt form under the name Fasudil, Monohydrochloride Salt, Cat. No. F-4660, as described on this page.
The monohydrochloride salt is the form used to prepare formulations of this drug for clinical use.  Note that the solubility properties of the mono- and di-HCl salts are different.
Kinase inhibitor; has antivasospastic properties.
Asano, T., et al.  "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinases."  Br. J. Pharmacol. 98:  1091-1100 (1989).
Sasaki, Y. and Sasaki, Y.  "Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator."  Biochem. Biophys. Res. Commun. 171:  1182-1187 (1990).
Seto, M., et al.  "Effects of HA 1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle."  Eur. J. Pharmacol. 195:  267-272 (1991).
Shibuya, O., et al.  The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:  53 (1988).
Shirotani, M. et al.  "A new type of vasodilator, HA 1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture."  J. Pharmacol. Exp. Ther. 259:  738-744 (1991).
Swärd, K. et al.  "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum."  J. Physiol. 522:  33-49 (2000).
Davies, S.P. et al.  "Specificity and mechanism of action of some commonly used protein kinase inhibitors."  Biochem. J. 351:  95-105 (2000).
This monohydrochloride salt form is the active ingredient in drug formulations marketed in Japan to treat cerebral vasospasm following surgery for subarachnoid hemorrhage and associated cerebral ischemic symptoms.  Zhao, J. et al.  "Effect of Fasudil Hydrochloride, a Protein Kinase Inhibitor, on Cerebral Vasospasm and Delayed Cerebral Ischemic Symptoms After Aneurysmal Subarachnoid Hemorrhage."  Neurologia Medico-Chirurgica 46:  421-428 (2006).  Also, the monohydrochloride form has been or presently is in human clinical trials for treatment of acute cerebral thrombosis, subarachnoid hemorrhage, and angina pectoris.
Related CAS numbers:  103745-39-7 for fasudil free base and 203911-27-7 for HA-1077 dihydrochloride salt.
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

 

 

 

-20 ºC.

F0275-1 g   Fasudil Hydrochloride   品牌 LKT

Fasudil Hydrochloride

货号: F0275-1 g      产品名称: Fasudil Hydrochloride   品牌: LKT 规格: 1 g 三周到货 生化试验

Fasudil Hydrochloride      
Description
is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. It has been found to be effective for the treatment of pulmonary hypertension. It was demonstrated in February of 2009 that Fasudil could also be used to enhance memory and improve the prognosis of Alzheimers patients.
Specifications 
Cas No. 105628-07-7
Product ID  F0275
Product Name  Fasudil Hydrochloride
Formula Wt. 327.83
Store Temp Ambient
"[Treatment of cerebral vasospasm by a protein kinase inhibitor AT 877]" (in Japanese). No to Shinkei 45 (9): 819–24. PMID 8217408. Doggrell SA (2005). "Rho-kinase inhibitors show promise in pulmonary hypertension.". Expert Opin Investig Drugs 14 (9): 1157–1159. doi:10.1517/13543784.14.9.1157. PMID 16144499. Huentelman, Matthew J.; Stephan, DA; Talboom, J; Corneveaux, JJ; Reiman, DM; Gerber, JD; Barnes, CA; Alexander, GE et al. (2009). "Peripheral delivery of a ROCK inhibitor improves learning and working memory". Behavioral Neuroscience 123 (1): 218. doi:10.1037/a0014260. PMID 19170447
 

室温

F0275-100 mg   Fasudil Hydrochloride   品牌 LKT

Fasudil Hydrochloride

货号: F0275-100 mg      产品名称: Fasudil Hydrochloride   品牌: LKT 规格: 100 mg 三周到货 生化试验

Fasudil Hydrochloride      
Description
is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. It has been found to be effective for the treatment of pulmonary hypertension. It was demonstrated in February of 2009 that Fasudil could also be used to enhance memory and improve the prognosis of Alzheimers patients.
Specifications 
Cas No. 105628-07-7
Product ID  F0275
Product Name  Fasudil Hydrochloride
Formula Wt. 327.83
Store Temp Ambient
"[Treatment of cerebral vasospasm by a protein kinase inhibitor AT 877]" (in Japanese). No to Shinkei 45 (9): 819–24. PMID 8217408. Doggrell SA (2005). "Rho-kinase inhibitors show promise in pulmonary hypertension.". Expert Opin Investig Drugs 14 (9): 1157–1159. doi:10.1517/13543784.14.9.1157. PMID 16144499. Huentelman, Matthew J.; Stephan, DA; Talboom, J; Corneveaux, JJ; Reiman, DM; Gerber, JD; Barnes, CA; Alexander, GE et al. (2009). "Peripheral delivery of a ROCK inhibitor improves learning and working memory". Behavioral Neuroscience 123 (1): 218. doi:10.1037/a0014260. PMID 19170447
 

室温

F0275-250 mg   Fasudil Hydrochloride   品牌 LKT

Fasudil Hydrochloride

货号: F0275-250 mg      产品名称: Fasudil Hydrochloride   品牌: LKT 规格: 250 mg 三周到货 生化试验

Fasudil Hydrochloride      
Description
is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. It has been found to be effective for the treatment of pulmonary hypertension. It was demonstrated in February of 2009 that Fasudil could also be used to enhance memory and improve the prognosis of Alzheimers patients.
Specifications 
Cas No. 105628-07-7
Product ID  F0275
Product Name  Fasudil Hydrochloride
Formula Wt. 327.83
Store Temp Ambient
"[Treatment of cerebral vasospasm by a protein kinase inhibitor AT 877]" (in Japanese). No to Shinkei 45 (9): 819–24. PMID 8217408. Doggrell SA (2005). "Rho-kinase inhibitors show promise in pulmonary hypertension.". Expert Opin Investig Drugs 14 (9): 1157–1159. doi:10.1517/13543784.14.9.1157. PMID 16144499. Huentelman, Matthew J.; Stephan, DA; Talboom, J; Corneveaux, JJ; Reiman, DM; Gerber, JD; Barnes, CA; Alexander, GE et al. (2009). "Peripheral delivery of a ROCK inhibitor improves learning and working memory". Behavioral Neuroscience 123 (1): 218. doi:10.1037/a0014260. PMID 19170447
 

室温