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TRV-120027 TFA

CAS No. :

MCE 站：TRV-120027 TFA

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：Angiotensin Receptor

In Vitro: TRV120027 TFA (100 nM) 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.
TRV120027 TFA (100 nM) 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.

In Vivo: TRV120027 TFA (intravenous injection; 0.3 or 1.5 µg/kg per minute; infusion rate, 0.5 mL/min) when added to furosemide decreases cardiac preload ａnd afterload, systemic ａnd renal vascular resistances, ａnd left ventricular external work while increasing cardiac output ａnd renal blood flow. GFR ａnd renal excretory function are maintained in canines with experimental HF.

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