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AMG9810

AMG9810是高效的,竞争性的香草素受体1选择性拮抗剂,对人类和大鼠TRPV1的IC50分别为24.5 和 85.6 nM。

CAS号

545395-94-6

分子式

C21H23NO3

主要靶点

TRP/TRPV Channel

仅限科研使用

Cat No : CM06797

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Synonyms

Transient receptor potential channels|TRPV Channel|TRPV1|TRPVChannel|TRPChannel|TRP Channel|Inhibitor|inhibit|(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺|AMG9810|AMG-9810|AMG 9810



产品信息

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat TRPV1, respectively).

CAS号 545395-94-6
分子式 C21H23NO3
主要靶点 TRP/TRPV Channel
主要通路 离子通道
分子量 337.41
纯度 99.95%, 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 Shipping with blue ice/Shipping at ambient temperature.
别名 Transient receptor potential channels|TRPV Channel|TRPV1|TRPVChannel|TRPChannel|TRP Channel|Inhibitor|inhibit|(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺|AMG9810|AMG-9810|AMG 9810

靶点活性

TRPV1 (human):24.5 nM |TRPV1 (rat):85.6 nM

体内活性

在通过足底注射完全弗氏佐剂引发的大鼠炎症痛模型中,30-100 mg/kg 的 AMG 9810 能逆转热和机械性高敏感症[3]。

溶解度

10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.93 mM);DMSO:117.5 mg/mL (348.24 mM)

参考文献

1.Mcdougle D R , Watson J E , Abdeen A A , et al. Anti-inflammatory ω-3 endocannabinoid epoxides[J]. Proceedings of the National Academy of Sciences, 2017:201610325.
2.Wolf F I , Vsimonacci T . Effect of transient receptor potential vanilloid 1 (TRPV1) receptor antagonist compounds SB705498, BCTC and AMG9810 in rat models of thermal hyperalgesia measured with an increasing-temperature water bath.[J]. European Journal of Pharmacology, 2010, 641(2):135-141.
3.Gavva NR, et al. AMG9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J Pharmacol Exp Ther. 2005 Apr;313(1):474-84.

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