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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

(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

验证数据展示

  • CAS No.: 545395-94-6

    AMG9810
    CAS#: 545395-94-6

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 98.00%， 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 (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

靶点活性

mTRPV1:85.6 nM|hTRPV1:24.5 nM

体内活性

In a rat model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia[3].

溶解度

DMSO:33 mg/mL (97.80 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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