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RQ-00203078

Chemical Structure : RQ-00203078

CAS No.: 1254205-52-1

RQ-00203078 (RQ00203078;RQ 00203078)

Catalog No.: PC-60787Not For Human Use, Lab Use Only.

A potent, selective and orally available TRPM8 channel inhibitor with IC50 of 8.3 nM (hTRPM8).

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

Biological Activity

A potent, selective and orally available TRPM8 channel inhibitor with IC50 of 8.3 nM (hTRPM8); inhibits rTRPM8 wiht IC50 of 5.8 nMdisplays no significant activities against TRPA1, TRPV4 and TRPV1 (IC50>3 uM); demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats; also reduces the invasion potential of oral squamous carcinoma cell lines.

Physicochemical Properties

M.Wt 554.844
Formula C21H13ClF6N2O5S
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

4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid

References

1. Okamoto Y, et al. Int J Oncol. 2012 May;40(5):1431-40.

2. Ohmi M, et al. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8.

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