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TRV-120027 TFA

TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂，可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂，可与 ß-arrestins 结合，同时阻断 G 蛋白信号传导。 它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌，并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。

CAS号

TP2158

分子式

C45H68F3N13O12

主要靶点

RAAS

仅限科研使用

Cat No : CM20646

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Synonyms

TRV-120027 TFA (1234510-46-3 free base)

验证数据展示

  • CAS No.: TP2158

    TRV-120027 TFA
    CAS#: TP2158

产品信息

TRV-120027 TFA is an angiotensin II–mediated vasoconstriction inhibitor and increases cardiomyocyte contractility. TRV-120027 TFA is a β-arrestin-1-biased AT1R agonist engaging ß-arrestins while blocking G-protein signaling[1]. TRV-120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling and promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane.

CAS号 TP2158
分子式 C45H68F3N13O12
主要靶点 RAAS
主要通路 内分泌与激素
分子量 1040.1
纯度 97.45%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 TRV-120027 TFA (1234510-46-3 free base)

靶点活性

the angiotensin II receptor type 1:

体内活性

TRV-120027 TFA combined with furosemide decreases cardiac preload and afterload, systemic and renal vascular resistances, and left ventricular external work while increasing cardiac output and renal blood flow[2].

体外活性

Treatment of 100 nM TRV-120027 TFA induces an [Ca2+]i increase in HEK293 cells co-transfected with AT1R, β-arrestin-1, and TRPC3, which are significantly blocked by Pyr3 pre-incubation in HEK293 cells co-transfected with Flag-AT1R-Cherry, HA-β-arrestin-1, and TRPC3-GFP[1]. Treatment of 100 nM TRV-120027 TFA significantly increases the AT1R and TRPC3 association with the immunoprecipitated β-arrestin-1 in HEK293 cells co-transfected with Flag-AT1R-cherry, HA-β-arrestin-1 and TRPC3-GFP[1].

溶解度

DMSO:88 mg/mL (84.61 mM)

参考文献

1.Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9;8:14335.
2.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.

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