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Submit ReviewRQ 00203078
Description: Potent and selective TRPM8 antagonist; orally active
Chemical Name: 4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid
Purity: ≥98% (HPLC)
Biological Activity for RQ 00203078
RQ 00203078 is a potent 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. Reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. Also attenuates icilin-induced wet dog shakes in rats. Orally active.
Compound Libraries for RQ 00203078
RQ 00203078 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for RQ 00203078
| M. Wt | 554.85 |
| Formula | C21H13ClF6N2O5S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1254205-52-1 |
| PubChem ID | 49783953 |
| InChI Key | IJGQFZYYEHCCIZ-UHFFFAOYSA-N |
| Smiles | ClC1=C(N(S(C3=CC=C(C(O)=O)C=C3)(=O)=O)CC2=CC=C(OC(F)(F)F)C=C2)N=CC(C(F)(F)F)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for RQ 00203078
References for RQ 00203078
References are publications that support the biological activity of the product.
Okamoto et al (2012) Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int.J.Oncol. 40 1431 PMID: 22267123
Ohmi et al (2014) Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg.Med.Chem.Lett. 24 5364 PMID: 25455182
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Keywords: RQ 00203078, RQ 00203078 supplier, RQ00203078, potent, selective, TRPM8, antagonists, transient, receptors, potential, channels, orally, active, melastatin-related, TRPM, 5388, Tocris Bioscience
2 Citations for RQ 00203078
Citations are publications that use Tocris products. Selected citations for RQ 00203078 include:
Martin F et al (2020) Mechanoactivation of NOX2-generated ROS elicits persistent TRPM8 Ca2+ signals that are inhibited by oncogenic KRas. Proc Natl Acad Sci U S A 117 26008-26019 PMID: 33020304
Gong and Jasmin (2017) Sustained MOR Administration Induces TRPM8-Dependent Cold Hyperalgesia. J Pain 18 212 PMID: 27845197
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