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Y-27632 2HCl 129830-38-2 Purity 99.96 China

Y-27632 2HCl
CAS: 129830-38-2
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Minimum Order Quantity:2 Metric Ton
Supply Ability:Metric Ton/Day
Updatetime:Mar 29 2019
Company Profile
Contact:Victor
Tel:86-021-68591985
Address: Room 207, Longzhu Square, No 2123, Pudong Ave
Quick Details
Classification: Biochemicals and biotech products
Cas NO.: 129830-38-2
Name: Y27632 (hydrochloride)
Molecular Formula: C14H23Cl2N3O
Melting Point: 258℃
Purity: 99.96
EINECS: 813-428-5
Purity: 99.96
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Detailed Description

Superiority

 

biological activity

description y-27632 2hcl is a selective rock1 (p160rock) inhibitor with ki of 140 nm, exhibits >200-fold selectivity over other kinases, including pkc, camp-dependent protein kinase, mlck and pak.
targets rock1 rock2        
ic50 140 nm (ki[1] 300 nm (ki[6]        
in vitro y-27632 2hcl inhibits rock-ii while displaying little activity against pkc, camp-dependent protein kinase and myosin light-chain kinase (mlck) with ki of 26 μm, 25 μm and > 250 μm, respectively, as well as pka activated by another rho-family gtpase member, cdc42. y-27632 2hcl inhibits smooth-muscle contraction induces by various agonists including phenylephrine, histamine, acetylcholine, serotonin, endothelin, and thromboxane with ic50 of 0.3-1 μm, by selectively inhibiting ca2+ sensitization. y-27632 2hcl suppresses rho-induced, p160rock-mediated formation of stress fibres in cultured cells. [1] y-27632 2hcl treatment blocks both rho-mediated activation of actomyosin and lpa-stimulated invasive activity of mm1 cells in a concentration-dependent manner. [2] y-27632 2hcl treatment is not only sufficient to initiate formation of exuberant axonal processes but also facilitates axonal maturation during the very early stages of axonogenesis, while largely sparing axon elongation. [3] in human embryonic stem (hes) cells, y-27632 2hcl treatment at 10 μm markedly diminishes dissociation-induced apoptosis even in serum-free suspension (sfeb) culture, increases cloning efficiency (from ~1% to ~27%), facilitates subcloning after gene transfer, and enables sfeb-cultured hes cells to survive and differentiate into bf1+ cortical and basal telencephalic progenitors. [4]
in vivo oral administration of y-27632 2hcl at 30 mg/kg significantly decreases the blood pressure in a dose-dependent manner in spontaneous hypertensive rats, renal hypertensive rats, as well as deoxycorticosterone acetate (doca)-salt hypertensive rats. [1] when y-27632 2hcl is continuously administered at a rate of 0.55 μl per hour by implanted pumps for 11 days tumor cell invasion (mm1 cells expressing val14-rhoa in rats) is significantly delayed. [2] by inhibiting rock, y-27632 2hcl treatment attenuates hypoxia-induced angiogenesis and vascular remodeling in the pulmonary circulation. [5]
features  

protocol(only for reference)

kinase assay: [1]

phosphorylation reactions the p160rock is expressed in cos cells as tagged full-length proteins, and immunoprecipitated by the use of anti-tag antibodies. the p160rock (30 ng) is incubated with 40 μm [γ-32p]atp (3.3 ci/mmol) and with 3 μg of either histone (hf2a), dephosphorylated casein or mbp in the presence of various concentrations of y-27632 2hcl at 30 °c in a total volume of 31 μl. a 7 μl aliquot is taken at 0, 5, 10, and 20 minutes, mixed with an equal volume of 2 × laemmli sample buffer, and applied to sds-page. the gel is stained with commassie blue, dried and subjected to analysis by a bioimage analyzer bas2000. the y-27632 2hcl concentration required to inhibit p160rock activity by 50% (ic50 value) is obtained. ki value is calculated according to the equation, ki = ic50/(1 + s/km), where s and km represent concentrations of and km value for atp.

animal study: [1]

animal models male wistar rats with spontaneous or induced hypertension
dosages 30 mg/kg/day
administration orally
solubility saline, 30 mg/ml

 

Details

Molecular Formula:C14H21N3O.2HCl
Keywords:ROCK1 inhibitor,p160ROCK inhibitor
Company Information
Name:Selleck China
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Trade Category: Trading Company
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Address: Room 207, Longzhu Square, No 2123, Pudong Ave
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Selleck(中国,上海蓝木化工有限公司)是美国Selleck Chemicals在上海设立的子公司,全权负责其全线产品在中国区域的销售。Selleck Chemicals是世界领先的高性能的生命科学产品供应商之一,主要致力于提供MAPK和PI3K/Akt/mTOR等上百个信号通路的高特异性小分子抑制剂。Selleck 产品线补充非常及时,可以提供行业内最新的抑制剂类产品。同时Selleck也是专业的高通量筛选抑制剂分子库、API、天然产物和多肽供应商。 Selleck的所有产品仅可用于科研目的的生物学实验(for research use only),严禁用于人体或动物的医疗目的。

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