CAS:659730-32-2AMG-517

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AMG-517 Cat No. FB06711Cas No. 659730-32-2

AMG-517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3234 mL
- 11.6170 mL
- 23.2340 mL
- 5 mM
- 0.4647 mL
- 2.3234 mL
- 4.6468 mL
- 10 mM
- 0.2323 mL
- 1.1617 mL
- 2.3234 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

659730-32-2

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C20H13F3N4O2S

运输

蓝冰

分子量

430.40

别名

溶解度

DMSO	86.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

10% Tween 80+water

30 mg/mL

suspension

靶点数据

生物活性

描述Vanilloid receptor-1 (TRPV1 or VR1), a well-characterized member of the transient receptor potential family of ion channels, has been implicated in the transmission of pain signaling. AMG 517, a compound that potently blocks multiple modes of TRPV1 activation, shows potency in the capsaicin- and acid-mediated assays with IC₅₀ values of 0.9 and 0.5 nM, respectively, while also processes excellent metabolic stability in human liver micosomes (CL_{in vitro} < 5 μl/min/mg). In the capsaicin-induced hypothermia model in rats, AMG 517 was effective in a rodent on-target biochemical challenge model (capsaicin-induced flinch, ED₅₀ = 0.33 mg/kg p.o.). In the complete Freund's adjuvant (CFA)-induced inflammatory pain model, AMG 517 showed dose-dependent inhibition of CFA-induced thermal hyperalgesia with efficacy at a minimum dose (MED) of 0.83 mg/kg (p.o.).
作用机制Hydrogen-bond donor−acceptor interactions between the carbonyl oxygen, NH proton, and the aromatic nitrogen of AMG 517 and the receptor are critical for its optimum potency.