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TRV-120027 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TRV-120027 TFA图片
规格:98%
分子量:1040.1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
TRV120027 TFA 是血管紧张素 II 受体 1 型 (AT1R) 的 β-arrestin-1 激动剂。TRV120027 TFA 通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌,促进质膜上 AT1R-β-arrestin-1-TRPC3-PLCγ 形成大分子复合物。TRV120027 TFA 抑制血管紧张素 II 介导的血管收缩并增加心肌细胞的收缩力。TRV120027 TFA有潜力用于急性失代偿性心力衰竭 (ADHF) 的研究。
货号:ajcx16664
CAS:N/A
分子式:C45H68F3N13O12
分子量:1040.1
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling[1]. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R-β-arrestin-1-TRPC3-PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment[2].


[1]. Boerrigter G, et al. TRV120027, a novel β-arrestin biased ligand at the angiotensin II type I receptor, unloads the heart and maintains renal function when added to furosemide in experimental heart failure.Circ Heart Fail. 2012 Sep 1;5(5):627-34. Epub 2012 Aug 13. [2]. Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9;8:14335.