AMG 9810 C화학적 특성, 용도, 생산
개요
AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC
50s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC
50s = 92.7 and 294 nM for human and rat, respectively), heat (IC
50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-
arachidonyl dopamine (IC
50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. 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.
용도
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, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. 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.[Cayman Chemical]
생물학적 활성
AMG 9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC 50 = 17 nM). Inhibits capsaicin-, proton-, heat- and endogenous ligand-induced activation of human and rat recombinant TRPV1 receptors. Displays antihyperalgesic properties in a rat model of inflammatory pain.
AMG 9810 준비 용품 및 원자재
원자재
준비 용품
