1470018-52-0
Chemical Structure
AMG2850
- CAS No.: 1470018-52-0
- Formula:C19H17F6N3O
- Molecular Weight:417.35
IUPAC Name: (R)-8-(4-(trifluoromethyl)phenyl)-N-((S)-1,1,1-trifluoropropan-2-yl)-5,8-dihydro-1,7-naphthyridine-7(6H)-carboxamide
InChIKey: DDBWYSSPWMXBIY-MEDUHNTESA-N
SMILES: O=C(N1CCC2=C(N=CC=C2)[C@H]1C3=CC=C(C(F)(F)F)C=C3)N[C@@H](C)C(F)(F)F
Biological Activity: AMG2850 is an orally active, blood-brain barrier-permeable selective TRPM8 competitive antagonist. AMG2850 abolishes the counterirritant effect of TRPM8 agonists, blocks TRPM8 activation induced by cold, (-)-Menthol (HY-75161) and Icilin (HY-11062), and exhibits selectivity over TRPA1, TRPV1, TRPV3 and TRPV4. AMG2850 is applicable for pain-related research[1][2][3][4].
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AMG2850 | 99.89% | AMG2850 is an orally active, blood-brain barrier-permeable selective TRPM8 competitive antagonist. AMG2850 abolishes the counterirritant effect of TRPM8 agonists, blocks TRPM8 activation induced by cold, (-)-Menthol (HY-75161) and Icilin (HY-11062), and exhibits selectivity over TRPA1, TRPV1, TRPV3 and TRPV4. AMG2850 is applicable for pain-related research. | ||||||||||||||||||||
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AMG2850 (Standard) | ≥98% | AMG2850 (Standard) is the analytical standard of AMG2850 (HY-104059). This product is intended for research and analytical applications. AMG2850 is an orally active, blood-brain barrier-permeable selective TRPM8 competitive antagonist. AMG2850 abolishes the counterirritant effect of TRPM8 agonists, blocks TRPM8 activation induced by cold, (-)-Menthol (HY-75161) and Icilin (HY-11062), and exhibits selectivity over TRPA1, TRPV1, TRPV3 and TRPV4. AMG2850 is applicable for pain-related research. | ||||||||||||||||||||
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References
- [1]. Ha MA, et al. Menthol attenuates respiratory irritation and elevates blood cotinine in cigarette smoke exposed mice. PloS one. 2015;10(2):e0117128. [Content Brief]
- [2]. Gavva NR, et al. Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Molecular pain. 2012 May 09;8:36. [Content Brief]
- [3]. Lehto SG, et al. AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia. Naunyn-Schmiedeberg's archives of pharmacology. 2015 Apr;388(4):465-76. [Content Brief]
- [4]. de Oliveira C, et al. Transient receptor potential channel ankyrin-1 is not a cold sensor for autonomic thermoregulation in rodents. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2014 Mar 26;34(13):4445-52.
