A-192621|195529-54-5|-陌孚医药/Medlife

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A-192621

目录号: PL13983 纯度: ≥99.0%

CAS No. :195529-54-5

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中文名称	A-192621
英文名称	A-192621
英文别名	3-Pyrrolidinecarboxylicacid,4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-,(2R,3R,4S)-;(2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(2,6-diethylanilino)-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid;3-Pyrrolidinecarboxylicacid,4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-,(2R,3R,;3-Pyrrolidinecarboxylicacid,4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-,[2R-(2a,3b,4a)]-;A 192621;A 192621.1;A-192621;A192621;5XE882529E;(2R,3R,4S)-4-(benzo[d][1,3]dioxol-5-yl)-1-(2-((2,6-diethylphenyl)amino)-2-oxoethyl)-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid;3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-(2-((2,6-diethylphenyl)amino)-2-oxoethyl)-2-(4-propoxyphenyl)-, (2R,3R,4S)-;(2R-(2alpha,3beta,4alpha)-4-(1,3-benzodioxol-5-yl)-1-(2-(2,6-diethylphenyl)amino)-2-oxoethyl)-2-(4-propoxyphenyl)-3-pyrrolidinecarboxylic acid;A-
Cas No.	195529-54-5
分子式	C₃₃H₃₈N₂O₆
分子量	558.66
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	A-192621 是一种有效的非肽，口服活性，选择性内皮素 B (ET_B) 受体拮抗剂，IC₅₀ 为 4.5 nM，K_i 为 8.8 nM。A-192621 的选择性比 ET_A 高 636 倍 (IC₅₀ 为 4280 nM，K_i 为 5600 nM)。A-192621 促进 PASMC 细胞凋亡，并引起动脉血压升高和血浆 ET-1 水平升高。
生物活性	A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ET B ) receptor antagonist with an IC 50 of 4.5 nM and a K i of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ET A (IC 50 of 4280 nM and K i of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
性状	Solid
IC50 & Target[1][2]	ETB 4.5 nM (IC50) ETBa
体外研究(In Vitro)	A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner. A-192621 (1-100 μM; 48 hours; PASMCs) treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs. A-192621 induces apoptosis in a dose-dependent manner and increases the cells susceptibility to apoptosis by Doxorubicin treatment. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ET B with an ED 50 value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ET A . A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Wu-Wong JR, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S. [2]. Sakai S, et al. Antagonists to endothelin receptor type B promote apoptosis in human pulmonary arterial smooth muscle cells. Life Sci. 2016 Aug 15;159:116-120.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (179.00 mM)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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