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JNJ-17203212

Chemical Structure : JNJ-17203212

CAS No.: 821768-06-3

JNJ-17203212 (JNJ17203212;JNJ 17203212)

Catalog No.: PC-42062Not For Human Use, Lab Use Only.

A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively; exhibits high selectivity against a panel of receptors and transporters, and does not inhibits related TRP channels TRPV2, TRPV4, or TRPA1; inhibits both pH (pIC50=7.23) and capsaicin (pIC50=6.32)-induced channel activation; attenuates capsaicin evoked coughs, prevents core hypothermia evoked by capsaicin in vivo.

Pain

Preclinical

Physicochemical Properties

M.Wt 419.3243
Formula C17H15F6N5O
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

1-Piperazinecarboxamide, 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-

References

1. Swanson DM, et al. J Med Chem. 2005 Mar 24;48(6):1857-72.

2. Bhattacharya A, et al. J Pharmacol Exp Ther. 2007 Nov;323(2):665-74.

3. Cefalu JS, et al. J Urol. 2009 Aug;182(2):776-85.

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