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1254205-52-1

1254205-52-1 structure
1254205-52-1 structure
  • Name: RQ 00203078
  • Chemical Name: rq-00203078
  • CAS Number: 1254205-52-1
  • Molecular Formula: C21H13ClF6N2O5S
  • Molecular Weight: 554.847
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
  • Create Date: 2016-02-08 10:22:19
  • Modify Date: 2024-02-04 19:04:52
  • 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: TRPM8in 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.

Name rq-00203078
Synonyms 4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid
RQ00203078
4-{[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][4-(trifluoromethoxy)benzyl]sulfamoyl}benzoic acid
Benzoic acid, 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-
Description 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: TRPM8in 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.
Related Catalog
Density 1.6±0.1 g/cm3
Boiling Point 602.0±65.0 °C at 760 mmHg
Molecular Formula C21H13ClF6N2O5S
Molecular Weight 554.847
Flash Point 317.9±34.3 °C
Exact Mass 554.013794
PSA 105.18000
LogP 6.04
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.567
Storage condition 2-8℃