A selective TRPM8 antagonist (IC50s = 8.3 and 5.8 nM in human and rat

RQ-00203078 – 1 mg

Brand:
Cayman
CAS:
1254205-52-1
Storage:
-20
UN-No:
Non-Hazardous - /

RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC50s = 8.3 and 5.8 nM in human and rat, respectively), while having little inhibitory action against TRPV1 (IC50 > 30 µM), TRPA1 (IC50 > 10 µM), TRPV4 (IC50 = 10 µM), or TRPM2 channels (IC50 > 10 µM).{31190} It attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg) after oral administration.{31190} RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.{31191} TRPM8, a member of the TRP melastatin subgroup, plays a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy, diabetic neuropathy, migraine, and overactive bladder. It is also known to be involved in the tumor progression of certain carcinomas.  

 

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Description

A selective TRPM8 antagonist (IC50s = 8.3 and 5.8 nM in human and rat, respectively); attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg); reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro

Formal name: 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-benzoic acid

Synonyms: 

Molecular weight: 554.8

CAS: 1254205-52-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Neuroscience|Pain Research

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