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TRV-120027 TFA

CAS号

分子式

C45H68F3N13O12

主要靶点

RAAS

仅限科研使用

Cat No : CM20646

Print datasheet

Synonyms

AT1 receptor|1234510-46-3|1234510-46-3 free base|the angiotensin II receptor type 1|TRP Channel|TRPVChannel|TRPV Channel|TRPChannel|TRV 120027 TFA|TRV120027 TFA|TRV-120027 TFA|TRV-120027 TFA (1234510-46-3 free base)

验证数据展示

  • CAS No.:

    TRV-120027 TFA
    CAS#:

产品信息

CAS号
分子式 C45H68F3N13O12
主要靶点 RAAS
主要通路 离子通道|G 蛋白偶联受体|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 keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 AT1 receptor|1234510-46-3|1234510-46-3 free base|the angiotensin II receptor type 1|TRP Channel|TRPVChannel|TRPV Channel|TRPChannel|TRV 120027 TFA|TRV120027 TFA|TRV-120027 TFA|TRV-120027 TFA (1234510-46-3 free base)

靶点活性

Ang II type 1 receptor:

体内活性

TRV-120027 TFA与呋塞米联合使用可降低心脏前负荷和后负荷、全身和肾脏血管阻力，并减少左心室外工作，同时增加心脏输出量和肾脏血流量[2]。

体外活性

处理100 nM TRV-120027 TFA可在共转染AT1R、β-arrestin-1和TRPC3的HEK293细胞中诱导[Ca2+]i增加，而在共转染Flag-AT1R-Cherry、HA-β-arrestin-1和TRPC3-GFP的HEK293细胞中经Pyr3预孵育显著阻断此增加[1]。此外，100 nM TRV-120027 TFA处理显著增加了共转染Flag-AT1R-cherry、HA-β-arrestin-1和TRPC3-GFP的HEK293细胞中AT1R和TRPC3与免疫沉淀的β-arrestin-1的结合[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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