Fasudil, a Rho-kinase inhibitor.

Fasudil, a Rho-kinase inhibitor, has been shown to reduce portal venous pressure in cirrhotic rats.

Product information

CAS Number: 103745-39-7

Molecular Weight: 291.37

Formula: C14H17N3O2S

Synonym:

AT877

HA1077

AT 877

AT-877

HA-1077

HA 1077

Related CAS Number:

105628-07-7 (Fasudil HCl)

Chemical Name: 5-(1, 4-diazepane-1-sulfonyl)isoquinoline

Smiles: O=S(=O)(C1=CC=CC2=CN=CC=C21)N1CCCNCC1

InChiKey: NGOGFTYYXHNFQH-UHFFFAOYSA-N

InChi: InChI=1S/C14H17N3O2S/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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Fasudil (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs and human HSC-derived TWNT-4 cells. Fasudil (50-100 μM; 24 hours) inhibits the LPA-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells. Fasudil (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells.

In Vivo:

Fasudil (intravenous injection; 0.01, 0.03, 0.1 and 0.3 mg/kg) decreases MBP and increases HR, VBF, CBF, RBF, and FBF. Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injur. Fasudil (orally administration; 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration.

References:

1. Li YH, Liu CY, Zhang PJ, Yu JZ, Ji N, Yan YY, Feng L, Zhang HF, Xiao BG, Ma CG. [Effect of Fasudil on miroglia and astrocytes in experimental autoimmune encephalomyelitis mice]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2012 Dec;28(12):1242-5. Chinese. PubMed PMID: 23232512.
2. Zeng P, Pi RB, Li P, Chen RX, Lin LM, He H, Zhou SY. Fasudil hydrochloride, a potent ROCK inhibitor, inhibits corneal neovascularization after alkali burns in mice. Mol Vis. 2015 Jun 12;21:688-98. eCollection 2015. PubMed PMID: 26120273; PubMed Central PMCID: PMC4463969.
3. Fukuda T, Narahara Y, Kanazawa H, Matsushita Y, Kidokoro H, Itokawa N, Kondo C, Atsukawa M, Nakatsuka K, Sakamoto C. Effects of fasudil on the portal and systemic hemodynamics of patients with cirrhosis. J Gastroenterol Hepatol. 2014 Feb;29(2):325-9. doi: 10.1111/jgh.12360. PubMed PMID: 24033356.
4. Ma ZP, Jiang R, Cheng Y, Yang HF, Chen F. [Fasudil improves erectile function of hypertensive rats]. Zhonghua Nan Ke Xue. 2012 Jan;18(1):11-5. Chinese. PubMed PMID: 22295842.
5. Watanabe G, Yamaguchi S, Tomita S, Nishida Y. Fasudil Is an Effective Graft Vasodilator for Gastroepiploic Artery in Coronary Artery Bypass Grafting. Innovations (Phila). 2015 Jul-Aug;10(4):268-72; discussion 272. doi: 10.1097/IMI.0000000000000178. PubMed PMID: 26360979.

Products are for research use only. Not for human use.