AMG517

AMG517

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 µM against TRPV2/3/4, TRPA1, and TRPM8-mediated responses; ﹤45% binding at 10 µM to 87 receptors, enzymes, and ion channels) and exhibits antihyperalgesic efficacy in vivo (capsaicin-induced flinch = ED50 = 0.33 mg/kg rats, p.o.; CFA-induced thermal hyperalgesia, MED = 0.83 mg/kg rats, p.o.).

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576723 AMG517 white to beige 100 SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£366.32 (exc VAT) per EACH
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3576724 AMG517 white to beige 100 SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£120.34 (exc VAT) per EACH
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