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RQ 00203078

Cat. No. 5388 1 Citation Submit a Review Datasheet / COA / SDS
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Cat.No. 5388 - RQ 00203078 | C21H13ClF6N2O5S | CAS No. 1254205-52-1
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)
Datasheet
Citations (1)
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

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Technical Data

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.48 100
ethanol 55.48 100

Preparing Stock Solutions

The following data is based on the product molecular weight 554.85. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.8 mL 9.01 mL 18.02 mL
5 mM 0.36 mL 1.8 mL 3.6 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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References

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

1 Citation for RQ 00203078

Citations are publications that use Tocris products. Selected citations for RQ 00203078 include:

Gong and Jasmin (2017) Sustained MOR Administration Induces TRPM8-Dependent Cold Hyperalgesia. J Pain 18 212 PMID: 27845197

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Literature in this Area

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Pain

Pain Research Product Guide

A collection of over 280 products for pain research, the guide includes research tools for the study of:

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Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.