U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C14H17N3O2S.ClH
Molecular Weight 327.83
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FASUDIL HYDROCHLORIDE

SMILES

Cl.O=S(=O)(N1CCCNCC1)C2=CC=CC3=C2C=CN=C3

InChI

InChIKey=LFVPBERIVUNMGV-UHFFFAOYSA-N
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

HIDE SMILES / InChI

Description

Fasudil is a potent Rho kinase inhibitor, which was developed by Asahi Kasei. The drug is used in Asia for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.4 µM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
ERIL

PubMed

Sample Use Guides

In Vivo Use Guide
The recommended dosage is 30 mg fasudil hydrochloride should be diluted in 50-100 mL solution and administered by intravenous infusion over 30 minutes 2-3 times daily.
Route of Administration: Intravenous
In Vitro Use Guide
The rat aortic rings were contracted by KCl; when the contraction reached a plateau, fasudil was added at concentrations from 10(-9) to 10(-5) M. The relaxation IC50 was 0.74 uM. When rabbit aortic rings were used, IC50 values were 37,15 uM and 27,54 uM for KCl and Methoxamine-induced contraction, respectively.