Basic Information

• Chinese Name: 盐酸法舒地尔

• English Name: Fasudil Hydrochloride

• CAS Number: 105628-07-7

• Molecular Formula: C14H18ClN3O2S (considering the hydrochloride salt)

• Molecular Weight: 327.83 g/mol (base compound) or 363.83 g/mol (including HCl)

Physical and Chemical Properties

• Melting Point: 208-215°C

• Boiling Point: 506.2°C at 760 mmHg (estimated)

• Flash Point: 259.9°C

• Solubility: Soluble in water and dimethyl sulfoxide, insoluble in ethanol

• Water Solubility: Greater than 200 mg/mL

• Refractive Index: 1.62 (estimated)

Structure and Synonyms

• Structural Formula: Contains an isoquinoline ring and sulfonyl group among other structural units

• Chinese Synonyms: 盐酸法苏地尔；六氢-1-(5-异喹啉磺酰基)-1H-1,4-二氮杂卓盐酸盐

• English Synonyms: Including 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride; 1-(5-Isoquinolinesulfonyl)homopiperazine Hydrochloride, among others

Pharmacological Effects

• Fasudil Hydrochloride is a non-specific RhoA/ROCK inhibitor and inhibits protein kinases. It has a Ki of 0.33 μM for ROCK1 inhibition and IC50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM for ROCK2, PKA, PKC, and PKG inhibition, respectively.

• It is also an effective Ca²⁺ channel antagonist and vasodilator.

Uses

• Fasudil Hydrochloride is primarily used in the treatment of angina pectoris and can be used to prevent and manage cardiovascular and cerebrovascular diseases.