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Fasudil hydrochloride

Fasudil hydrochloride structure

CAS No:
105628-07-7
Formula:
C14H17N3O2S.ClH
Chemical Name:
Fasudil hydrochloride
Synonyms:
Isoquinoline,5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-,hydrochloride (1:1);1H-1,4-Diazepine,hexahydro-1-(5-isoquinolinylsulfonyl)-,monohydrochloride;1-(5-Isoquinolinesulfonyl)homopiperazine hydrochloride;Eril;Fasudil hydrochloride
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Fasudil hydrochloride, a novel calcium antagonistic vasodilator, was marketedfor the treatment of cerebral vasospasm following subarachnoid hemorrhage(SAH). Fasudil is also a potent inhibitor of myosin light chain kinase and protein kinaseC. In contrast to other calcium channel blockers, which regulate the influx of calciumions through the cell membrane but not involved in the intracellular regulatorymechanism of the calcium, fasudil was suggested to have an intracellular mode ofact

Fasudil hydrochloride is a member of isoquinolines and a N-sulfonyldiazepane.

Fasudil hydrochloride Basic Attributes

Molecular Weight：

327.83

Exact Mass：

327.081

EC Number：

1308068-626-2

UNII：

SQ04N8S7BR

DSSTox ID：

DTXSID1045615

HScode：

29339900

Characteristics

PSA：

70.7

XLogP3：

4.17030

Appearance：

white solid

Melting Point：

220 °C (approx)

Boiling Point：

506.2ºC at 760 mmHg

Flash Point：

259.9ºC

Water Solubility：

soluble in water and dimethyl sulfoxide. Insoluble in ethanol.

Toxicity：

LD50 in mice, rats (mg/kg): 67.5, 59.9 i.v.; 124.5, 123.2 s.c.; 273.9, 335.0 orally (Koga)

Safety Information

wgk germany：

hazard class code：

safety instructions：

36-60

RTECS Number：

HM4031166

Precautionary statement(s)：

P264, P270, P301+P312, P330, P501

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

Drug Indication：

Treatment of non-traumatic subarachnoid haemorrhage

MeSH：

Agents that inhibit PROTEIN KINASES. (See all compounds classified as Protein Kinase Inhibitors.)|A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)|Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

MeSH Entry Terms：

1-(5-isoquinolinesulfonyl)homopiperazine

Fasudil hydrochloride Use and Manufacturing

Uses

vasodilator, potent Rho-kinase inhibitor Cardiovascular and cerebrovascular drugs, used to improve the symptoms of ischemic cerebrovascular disease caused by cerebral vasospasm after subarachnoid hemorrhage; an effective Rho kinase inhibitor and vasodilator. It also has inhibitory activity on PKA, PKG, PKC and MLCK.

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:327.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:2
Exact Mass:327.0808257
Monoisotopic Mass:327.0808257
Topological Polar Surface Area:70.7
Heavy Atom Count:21
Complexity:421
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Unspecified

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

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Registered Holders

Tianjin Zhongrui Pharmaceutical Co., Ltd.

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