AMG2850

Product details

• Chemical name: ((R)-8-(4-(trifluoromethyl)phenyl)-N-((S)-1,1,1-trifluoropropan-2-yl)-5,6-dihydro-1,7-naphthyridine-7(8H)-carboxamide).
• CAS number: 1470018-52-0
• Molecular formula: C19H17F6N3O.
• Purity: >99% (HPLC)
• Concentration: 0.1-10 µM.
• Form: Lyophilized Powder
• Solubility: Up to 200 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
• Reconstitution: Up to 200 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: TRPM8 channel
• Source: Synthetic
• Activity: AMG2850 is a potent and selective blocker of TRPM8 channels. It was shown in vitro to inhibit rat TRPM8 cold, menthol and icilin activation with IC50 of 7.3 nM, 156 nM and 204 nM, respectively. Highly selective for TRPM8 over TRPV1 and TRPA1 channels and orally bioavailable (Fpo>40%)1,2.

Scientific background

AMG2850 is a selective blocker of TRPM8 channels. The compound shows high selectivity towards TRPM8 over TRPV1 and TRPA1 channels. AMG2850 potently inhibits the menthol and cold-induced increase in intracellular Ca2+ in cells expressing rat TRPM8. In vitro, it was shown to inhibit rat TRPM8 against cold, menthol and icilin activation with IC50 of 7.3 nM, 156 nM and 204 nM, respectively1,2. AMG2850 is orally bioavailable and its plasma half-life (T1/2) in rats is 3.5 hours1,2.TRPM8 is a Ca2+-permeable channel, a member of the 'long' or melastatin (M) group of TRP channels and is activated by temperatures in the range of 8-28°C or by cooling compounds such as icilin. The TRPM8 gene is expressed and up-regulated in prostate cancer and other malignancies. TRPM8 channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons3,4.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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