Fasudil

Cas：103745-39-7

Product Information：

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

Chemical Formula: C14H17N3O2S

Exact Mass: 291.1041

Molecular Weight: 291.369

Elemental Analysis: C, 57.71; H, 5.88; N, 14.42; O, 10.98; S, 11.00

Synonym:

AT877

HA1077

Chemical Name:

1H-1,4-Diazepine, hexahydro-1-(5-isoquinolinylsulfonyl)-

InChi Key:

NGOGFTYYXHNFQH-UHFFFAOYSA-N

InChi Code: 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

Smiles Code:

O=S(N1CCNCCC1)(C2=CC=CC3=C2C=CN=C3)=O

Technical Data：

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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.