HA-1077 (hydrochloride) - CAS:203911-27-7

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HA-1077 (hydrochloride) (Synonyms:法舒地尔二盐酸盐; HA-1077 dihydrochloride; AT-877 dihydrochloride;Fasudil dihydrochloride)

目录号 : KCM12418 CAS No. : 203911-27-7 纯度 : ≥98%

Data Sheet 产品使用指南

Rho-associated kinase (ROCK), an effector of the small GTP-binding protein Rho, plays an important role in various cellular functions including vascular smooth muscle contraction, proliferation, and migration as well as inflammatory cell mobility. HA-1077 is a potent inhibitor of ROCK2 and additionally inhibits protein kinase c-related kinase 2 (PRK2), mitogen- and stress-activated protein kinase (MSK1), and mitogen activated protein kinase-activated protein kinase 1b (MAPKAP-K1b) with IC values of 1.9, 4, 5, and 15 µM, respectively. By inhibiting the activity of ROCK, HA-1077 has been shown to reduce blood vessel constriction, decrease pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in various rodent models. While originally marketed for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage, oral formulations of HA-1077 are used for the treatment of a wide range of cardiovascular diseases including pulmonary arterial hypertension and stable angina.

规格	价格	是否有货	数量
25mg		In-stock
50mg		In-stock
100mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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生物活性

HA-1077 (hydrochloride) is a nonspecific RhoA/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. HA-1077 (hydrochloride) is also a potent Ca2+ channel antagonist and vasodilator.

体外研究

HA-1077 (hydrochloride) (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells.
HA-1077 (hydrochloride) (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells.
HA-1077 (hydrochloride) (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells.

Western Blot Analysis

Cell Line:	Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:	50 μM; 100 μM
Incubation Time:	24 hours
Result:	Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively.

RT-PCR

Cell Line:	Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:	25 μM; 50 μM; 100 μM
Incubation Time:	24 hours
Result:	Reduced the expression of type I collagen, a-SMA, and TIMP-1.

体内研究

HA-1077 (hydrochloride) (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury.
HA-1077 (hydrochloride) (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio.
HA-1077 (hydrochloride) (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice.

Animal Model:

Myocardial ischemia and reperfusion in rat (250-300 g)

Dosage:

10 mg/kg

Administration:

Intravenous injection; 1 h before operation

Result:

Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus.
Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis.

分子式

C₁₄H₁₇N₃O₂S^.₂HCl

分子量

364.29

CAS号

203911-27-7

中文名称

法舒地尔二盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H2O : ≥ 100 mg/mL (274.51 mM)

DMSO : 20.83 mg/mL (57.18 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7451 mL	13.7253 mL	27.4507 mL
5 mM	0.5490 mL	2.7451 mL	5.4901 mL
10 mM	0.2745 mL	1.3725 mL	2.7451 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： ≥98%