Z62954982

生物活性体外研究体内研究

Z62954982

CAS号:: 1090893-12-1

英文名:: Rac1 Inhibitor II

英文别名:: Rac1 Inhibitor II;Z-62954982,Z62954982;Z62954982 (Synonyms: ZINC08010136);Rac1 Inhibitor II - CAS 1090893-12-1 - Calbiochem;InSolution Rac1 Inhibitor II, Z62954982 - CAS 1090893-12-1 - Calbiochem;Benzamide, N-[3-(aminosulfonyl)-4-methylphenyl]-3-[(3,5-dimethyl-4-isoxazolyl)methoxy]-

中文名:: Z62954982

中文别名:

CBNumber:: CB92684115

分子式:: C20H21N3O5S

分子量:: 415.46

MOL File:: 1090893-12-1.mol

化学性质安全信息用途供应商 9

Z62954982化学性质

储存条件:: -20C

溶解度:: Soluble in DMSO

形态:: Off-white solid

安全信息

Z62954982性质、用途与生产工艺

生物活性

Z62954982 (ZINC08010136) 是一种强效的、选择性的、细胞渗透性强的 Rac1 (IC50=12 μM) 抑制剂，比 NSC23766 (HY-15723A) (IC50=50 μM) 有效性强 4 倍。Z62954982 干扰 Rac1/Tiam1 复合物，降低活性 Rac1 (GTP 结合的 Rac1) 的细胞质水平，而不影响其他 Rho GTPases (如，Cdc42 或 RhoA) 的活性。

体外研究

Z62954982 (5-100 μM; 4 hours) reduces the intracellular levels of Rac1- GTP in a concentration-dependent manner,and shows the most potent inhibitory action with an IC ₅₀ of 12.2 μM in Human SMCs.Z62954982 (25 μM; 4 hours) significantly reduces the ratio Rac1-GTP/Rac1 and has the most potent inhibitory action (86.0%) in cultured SMCs.Z62954982 (10-100 μM; 72 hours) causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC monolayers.

体内研究

Z62954982 (intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks) has no obvious signs of toxicity and decreases both phosphorylation of p38 as well as secreted IL-6 in PASMCs in response to hypoxia in both abr ^-/- and bcr ^-/- mice.

Animal Model:	Male bcr ^-/- , abr ^-/- and wt mice (8 to 10-week-old littermates) are exposed to hypoxia (10% O2) or normoxia (21% O2) for 3 weeks
Dosage:	10 mg/kg or 20 mg/kg
Administration:	Intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks
Result:	Promoted phosphorylation of p38 MAPK and increased IL-6 in Hypoxia in mice.

Z62954982 上下游产品信息

上游原料

下游产品

Z62954982 生产厂家

全球有 9家供应商 Z62954982国内生产厂家

供应商	联系电话	电子邮件	国家	产品数	优势度
Sigma-Aldrich西格玛奥德里奇(上海)贸易有限公司	021-61415566 800-8193336	orderCN@merckgroup.com	中国	51471	80
上海源溪生物科技有限公司	021-58447131 13564518121	sales@dcchemicals.com	中国	9414	58
苏州优睿科化工医药科技有限公司	15317229551	15151849396@163.com	中国	997	58
上海传芊化工科技中心	15869524721	3525679403@qq.com	中国	3915	58
TargetMol中国（陶术生物）	4008200310	marketing@tsbiochem.com	中国	24131	58
南通全益生物科技有限公司	0513-66337626 18051384581	sales@chemhifuture.com	中国	4030	58
銳迪國際科技有限公司	18988968278	sales@ubiochem.com	中国	9146	58

1090893-12-1, Z62954982 相关搜索:

1090893-12-1
Z-62954982,Z62954982
Z62954982 (Synonyms: ZINC08010136)
Benzamide, N-[3-(aminosulfonyl)-4-methylphenyl]-3-[(3,5-dimethyl-4-isoxazolyl)methoxy]-
InSolution Rac1 Inhibitor II, Z62954982 - CAS 1090893-12-1 - Calbiochem
Rac1 Inhibitor II - CAS 1090893-12-1 - Calbiochem
Rac1 Inhibitor II