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RQ 00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively). Exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. Reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. Also attenuates icilin-induced wet dog shakes in rats. Orally active.
| Molecular Weight | 554.85 |
| Formula | C21H13ClF6N2O5S |
| CAS Number | 1254205-52-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related TRP Channel Products |
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| PF-04745637
PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1. |
| Phenazopyridine
Phenazopyridine is a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine can promote neuronal differentiation and it can also be used in the research of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases. |
| 4-ONE
4-ONE is one of the major hemolytic decomposition products of lipid hydroperoxides. 4-ONE is a potent transient receptor potential ankyrin 1 (TRPA1) agonist. |
| Moringin
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. |
| (S)-ABT-102
(S)-ABT-102 is a potent TRPV1 antagonist, with an IC50 of 123 nM. (S)-ABT-102 can block the activation of TRPV1 by capsaicin. |
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