Chemical Name |
RQ-00203078 |
CAS Number |
1254205-52-1 |
Molecular Formula |
C21H13ClF6N2O5S |
Molecular Weight |
554.85 |
Introduction of 1254205-52-1 :
RQ-00203078 is a highly selective, potent and orally available 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. IC50 value: 5.3 nM (for rat channel), 8.3 nM nM ( for human channel) Target: TRPM8 in vitro: RQ-00203078 reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion. in vivo: RQ-00203078 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 after oral administration and may become an important pharmacological tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation. RQ-00203078 also attenuates icilin-induced wet dog shakes in rats.
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.