AMG2850 (AMG-2850)

Chemical Structure : AMG2850

CAS No.: 1470018-52-0

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货号: PC-28382Not For Human Use, Lab Use Only.

AMG2850 is a potent and selective antagonists of TRPM8, potently inhibits menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8 with IC50 of 156 nM.

规格	价格	库存
5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3480	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

AMG2850 is a potent and selective antagonists of TRPM8, potently inhibits menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8 with IC50 of 156 nM.
AMG2850 is selective for TRPM8 relative to the recombinant TRP family members TRPA1, capsaicin activated TRPV1, 2-Aminoethoxydiphenyl borate activated TRPV3, and 4α-phorbol 12, 13-didecanoate activated TRPV4.
AMG2850 is potent in vitro at rat TRPM8 (IC90 against icilin activation of 204 ± 28 nM), highly selective (>100-fold IC90 over TRPV1 and TRPA1 channels), and orally bioavailable (F po > 40 %).
AMG2850 blocks menthol-induced action potentials but not mechanical activation in C fibers.
AMG2850 exhibits significant target coverage in vivo in a TRPM8-mediated icilin-induced wet-dog shake (WDS) model in rats (at 10 mg/kg p.o.).

物理化学性质&存储条件

分子量	417.36
分子式	C19H17F6N3O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-8-(4-(Trifluoromethyl)phenyl)-N-((S)-1,1,1-trifluoropropan-2-yl)-5,8-dihydro-1,7-naphthyridine-7(6H)-carboxamide

参考文献

1. Gavva NR, et al. Mol Pain. 2012 May 9;8:36.

2. Liu B, et al. Pain. 2013 Oct;154(10):2169-2177.

3. Lehto SG, et al. Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):465-76.

AMG2850 (AMG-2850)

生物&药学活性

物理化学性质&存储条件

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AMG2850 (AMG-2850)

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