2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. 1254205-52-1

1254205-52-1

RQ-00203078 Chemical Structure

1254205-52-1

Chemical Structure

  • RQ-00203078
  • CAS No: 1254205-52-1
    Formula: C21H13ClF6N2O5S
    Molecular Weight: 554.85
  • IUPAC Name: 4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid
  • InChIKey: IJGQFZYYEHCCIZ-UHFFFAOYSA-N
  • SMILES: O=C(O)C1=CC=C(S(=O)(N(C2=NC=C(C(F)(F)F)C=C2Cl)CC3=CC=C(OC(F)(F)F)C=C3)=O)C=C1

Biological Activity: RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels[1][2].

Cat. No. Product Name Purity Description
HY-18662 RQ-00203078 99.62% RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.

References

[1]. Masashi Ohmi, et al. Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8. [Content Brief]
[2]. Yoshihiko Okamoto, et al. Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int J Oncol. 2012 May;40(5):1431-40. [Content Brief]

Keywords:

RQ-00203078