AMG-9810

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、竞争性的 TRPV1 拮抗剂，对人和大鼠 TRPV1 的 IC50 值分别为 24.5 和 85.6 nM。

A potent, selective and competitive TRPV1 antagonist with IC50 of 24.5 and 85.6 nM for human and rat TRPV1, repectively; blocks capsaicin-evoked depolarization and CGRP release in cultures of rat dorsal root ganglion primary neurons; the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain.Pain Preclinical.

AMG9810 is a competitive antagonist of capsaicin activation (IC50 value for human TRPV1, 24.5±15.7 nM; rat TRPV1, 85.6±39.4 nM) and blocks all known modes of TRPV1 activation, including protons (IC50 value for rat TRPV1, 294±192 nM; human TRPV1, 92.7±72.8 nM), heat (IC50 value for rat TRPV1, 21±17 nM; human TRPV1, 15.8±10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. AMG9810 inhibits capsaicin-, proton-, heat-, and endogenous ligand-induced uptake of 45Ca2+ into TRPV1-expressing cells.

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. At effective doses, AMG9810 does not show any significant effects on motor function. AMG9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain. AMG9810, promotes mouse skin tumor development. 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.

AMG9810 | AMG 9810

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

Neurological Disease

Pain

545395-94-6

337.42

C21H23NO3

>98% (HPLC)

DMSO: ≥ 33 mg/mL

CC(C)(C)c1ccc(cc1)/C=C/C(=O)Nc2ccc3c(c2)OCCO3

2-Propenamide, N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-, (2E)-

(-20℃)

With Ice Pack

≥ 2 years