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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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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. |
Oleoyl Serotonin
Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1. |
ABT-102
ABT-102 (CHEMBL398338) is a potent and highly selective transient receptor potential vanilloid 1 (TRPV1) receptor antagonist. |
MK-2295
MK-2295 (TRPV1 antagonist 5) is a potent TRPV1 antagonist. MK-2295 can be used for the research of chronic pain. |
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