化合物 Fasudil dihydrochloride,Fasudil dihydrochloride

化合物 Fasudil dihydrochloride|T61382|TargetMol

價(jià)格	￥2640	￥1690	￥770
包裝	100mg	50mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 Fasudil dihydrochloride	英文名稱:Fasudil dihydrochloride
CAS:203911-27-7	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Shipping with blue ice.
產(chǎn)品類別: 抑制劑
貨號(hào): T61382

Product Introduction

Bioactivity

名稱	Fasudil dihydrochloride
描述	Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3].
體外活性	Fasudil dihydrochloride (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 [4]. Fasudil dihydrochloride (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 [4]. Fasudil dihydrochloride (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells [4]. Western Blot Analysis [4] 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 [4] 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.
體內(nèi)活性	Fasudil dihydrochloride (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 [5]. Fasudil dihydrochloride (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 [6]. Fasudil dihydrochloride (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 [6]. Animal Model: Myocardial ischemia and reperfusion in rat (250-300 g) [5] 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.
存儲(chǔ)條件	Shipping with blue ice.

關(guān)鍵字： Fasudil dihydrochloride|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.265100萬(wàn)人民幣
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