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RQ 00203078
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C21H13ClF6N2O5S
- MW: 554.85
Description
RQ 00203078 is a selective and orally active antagonist of TRPM8 ion channels with potent in vitro and in vivo activity. It blocks TRPM8-mediated cold-sensing responses and reduces icilin-induced behaviors in preclinical models.
TRPM8 is a thermosensory cation channel involved in cold sensation, nociception and sensory neuron excitability. RQ 00203078 is useful for evaluating TRPM8 antagonism in pain, thermoregulation and sensory pharmacology studies.
Key Features
- Potent TRPM8 antagonist
- Reported IC50: 8.3 nM
- Orally active with reported ED50: 0.65 mg/kg in an icilin-induced wet-dog-shake model
- Selective pharmacology for cold-sensing ion-channel studies
Applications
- TRPM8 ion-channel research
- Cold pain and sensory neuron studies
- In vivo thermosensation models
- Analgesic pathway pharmacology
More Information
| Parent CAS No. | 1254205-52-1 |
|---|---|
| Chemical Name | 4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid |
| SMILES | C(O)(=O)C1=CC=C(S(N(C2=NC=C(C(F)(F)F)C=C2Cl)CC2=CC=C(OC(F)(F)F)C=C2)(=O)=O)C=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C21H13ClF6N2O5S/c22-17-9-14(20(23,24)25)10-29-18(17)30(11-12-1-5-15(6-2-12)35-21(26,27)28)36(33,34)16-7-3-13(4-8-16)19(31)32/h1-10H,11H2,(H,31,32) |
| InChiKey | IJGQFZYYEHCCIZ-UHFFFAOYSA-N |
| CID | 49783953 |
| Short Description | TRPM8 antagonist |
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