|(E)-3-(4-(叔丁基)苯基)-N-(2,3-二羟基苯并[b][1,4]二氧杂环己烷基-6-基)丙烯酰胺|CsnPharm

CAS No.: 545395-94-6

AMG9810 Catalog No. CSN21956

Synonyms: (2E)-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-3-[4-(1,1-DIMETHYLETHYL)PHENYL]-2-PROPENAMIDE

AMG9810 is an antagonist of TRPV1 receptor with IC50 of 17 nM and exhibits antihyperalgesic properties in rat model.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The vanilloid receptor 1 (TRPV1) is a membrane-bound, nonselective cation channel expressed by peripheral sensory neurons^[2]. AMG9810 is a selective and competitive TRPV1 antagonist with IC₅₀ values of 24.5 ± 15.7 and 85.6 ± 39.4 nM for human and rat TRPV1, repectively. AMG9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. In addition, it inhibits capsaicin-, proton-, heat-, and endogenous ligand-induced uptake of ⁴⁵Ca²⁺ into TRPV1-expressing cells^[2]. AMG9810 is effective at preventing capsaicin-induced eye wiping in a dose-dependent manner, and it reverses thermal and mechanical hyperalgesia in a model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant^[2]. The topical application of AMG9810 results in a significant increase in the expression level of the epidermal growth factor receptor (EGFR) and its downstream Akt/mammalian target of rapamycin (mTOR)-signaling pathway^[3].
参考文献

[1] Gavva NR, Tamir R, Qu Y, Klionsky L, Zhang TJ, Immke D, Wang J, Zhu D, Vanderah TW, Porreca F, Doherty EM, Norman MH, Wild KD, Bannon AW, Louis JC, Treanor JJ. AMG 9810 [(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. doi: 10.1124/jpet.104.079855. Epub 2004 Dec 22. PMID: 15615864.
[2] Li S, Bode AM, Zhu F, Liu K, Zhang J, Kim MO, Reddy K, Zykova T, Ma WY, Carper AL, Langfald AK, Dong Z. TRPV1-antagonist AMG9810 promotes mouse skin tumorigenesis through EGFR/Akt signaling. Carcinogenesis. 2011 May;32(5):779-85. doi: 10.1093/carcin/bgr037. Epub 2011 Feb 23. PMID: 21349818; PMCID: PMC3086704.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9637 mL
- 14.8187 mL
- 29.6373 mL
- 5 mM
- 0.5927 mL
- 2.9637 mL
- 5.9275 mL
- 10 mM
- 0.2964 mL
- 1.4819 mL
- 2.9637 mL

技术信息

CAS号

545395-94-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H23NO3

运输

蓝冰

分子量

337.41

别名

(2E)-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-3-[4-(1,1-DIMETHYLETHYL)PHENYL]-2-PROPENAMIDE

溶解度

DMSO	240.0 mg/mL (711.3 mM)
Water	insoluble

动物实验配方

5% DMSO + 30%PEG400 +10% Tween80 + water

5 mg/mL

clear

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