Fasudil(HA-1077)HCl

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Fasudil(HA-1077)HCl

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	105628-07-7
规格:	≥98%

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议
1g	电议
2g	电议
5g	电议

产品介绍

Fasudil HCl (formerly known as HA1077; HA 1077; HA-1077), the hydrochloride salt of fasudil, is a potent multikinase inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with the potential to be used for the treatment of cerebral vasospasm. It is also a promising drug candidate for a disease-modifying therapy of amyotrophic lateral sclerosis (ALS). Fasudil inhibits ROCK-II, PKA, PKG, PKC, and MLCKwith Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM in cell-free assays, respectively. It is used as a vasodilator for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. Fasudil is found to be effective for the treatment of pulmonary hypertension.

理化性质和储存条件

Molecular Weight (MW)	327.83
Formula	C14H17N3O2S.HCl
CAS No.	105628-07-7
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 5 mg/mL (15.3 mM)
	Water: 65 mg/mL (198.3 mM)
	Ethanol:<1 mg/mL
Solubility (In vivo)	Saline: 30 mg/mL
Synonyms	HA-1077 HCl; HA-1077; Fasudil hydrochloride; HA1077; HA 1077

实验参考方法

In Vitro	In vitro activity: Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. Fasudil induces disorganization of actin stress fiber and cell migration inhibition. Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. Kinase Assay: Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Cell Assay: In oral squmous cell carcinoma SCC-4 cells, administration of Fasudil (HA-1077) HCl markedly decreases cell motility and inhibits cell migration or invasion in a dose dependent manner (1, 50 and 100 μmol/L.
In Vivo	Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil 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 significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice.
Animal model	Dogs
Formulation & Dosage	0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.
References	Nature. 1997 Oct 30;389(6654):990-4; Nat Med. 1999 Feb;5(2):221-5.