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JNJ 41876666

Chemical Structure : JNJ 41876666

CAS No.: 1259026-14-6

JNJ 41876666 (JNJ-41876666;JNJ41876666)

Catalog No.: PC-60719Not For Human Use, Lab Use Only.

A potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM, .

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM, ; exhibits minimal effect on the enzyme activity of CYP isoforms 3A4, 1A2, 2D6, 2C9, and 2C19 (IC50>10 uM); completely prevents icilin-induced WDS at an oral dose of 10 mg/kg, exhibits potent in vitro functional activity and robust oral efficacy in an inflammatory model of neuropathic pain at relatively low plasma levels; also reduces proliferation rates and proliferative fraction in prostate cancer cells.

Physicochemical Properties

M.Wt 503.873
Formula C23H20ClF6N3O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[7-Trifluoromethyl-5-(2-trifluoromethyl-phenyl)-1H-benzimidazol-2-yl]-1-oxa-2-aza-spiro[4.5]dec-2-ene hydrochloride

References

1. Valero ML, et al. PLoS One. 2012;7(12):e51825.

2. Parks DJ, et al. J Med Chem. 2011 Jan 13;54(1):233-47.

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