Name: RQ-00203078
Price: 276.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Description:IC50: 8.3 and 5.8 nM for hTRPM8 and rTRPM8, respectivelyThe transient receptor potential melastatin 8 (TRPM8), a member of the TRP melastatin sub-group, is known to play a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy (CIPN, using the agents oxaliplatin, vincristine, or paclitaxel), diabetic neuropathy, migraine and overactive bladder (OAB). RQ-00203078 is identified as a selective and orally active TRPM8 antagonist.In vitro: In the menthol-induced calcium influx assay, RQ-00203078 is a novel and highly potent TRPM8 antagonist with human and rat IC50 values of 8.3 nM and 5.8 nM, respectively. RQ-00203078 was highly selective over other TRP channels [1]. In vivo: RQ-00203078 demonstrated excellent activity in vivo 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 [1]. Clinical trial: Up to now, RQ-00203078 is still in the preclinical development stage.
- Properties
  - Categories
    
    Selective and orally active TRPM8 antagonist
    
    Alternative Name
    
    4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid
    
    CAS Number
    
    1254205-52-1
    
    Molecular Formula
    
    C21H13ClF6N2O5S
    
    Molecular Weight
    
    554.85
    
    Appearance
    
    A solid
    
    Purity
    
    99.38%
    
    Solubility
    
    insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥27.25 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    ClC1=C(N(CC2=CC=C(OC(F)(F)F)C=C2)S(C3=CC=C(C(O)=O)C=C3)(=O)=O)N=CC(C(F)(F)F)=C1
    
    * For Research Use Only
- Reference
  - 1. Lan X, Zhao J, et al. "TRPM8 facilitates proliferation and immune evasion of esophageal cancer cells." Biosci Rep. 2019 Sep 13. pii: BSR20191878. PMID:31519770