Synonyms: AMG 517; AMG-517; N-(4-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-yloxy)benzo[d]thiazol-2-yl)acetamide; N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide
Molecular Formula: C20H13F3N4O2S
Molecular Weight: 430.4
Linear Structural Formula: C20H13F3N4O2S
MDL Number: MFCD14584859
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: AMG517 is an orally active, highly potent and selective vanilloid receptor-1 (TRPV1; VR1; capsaicin receptor) antagonist that blocks TRPV1-mediated cellular Ca2+ influx (h/r/m IC50/stimulant = 0.76 nM/1.01 nM/1.9 nM/500 nM capsaicin; 0.62 nM/0.5 nM/0.63 nM/acid (pH 5) using respective CHO transfectants; IC50 >20 muM against TRPV2/3/4, TRPA1, and TRPM8-mediated responses;<45 % binding at 10 mum to 87 receptors, enzymes, and ion channels) and exhibits antihyperalgesic efficacy in vivo (capsaicin-induced flinch="ED50" 0.33 mg g rats, p.o.; cfa-induced thermal hyperalgesia, med="0.83" mg g rats, p.o.).<>