RQ 00203078

Name: RQ 00203078
Brand: Tocris Bioscience
SKU: 5388

Tocris Bioscience, part of Bio-Techne | Catalog # 5388

Citations (6)

COA / SDS

Potent and selective TRPM8 antagonist; orally active

Key Product Details

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)
Molecular Weight:	554.85

View Full Technical Details for RQ 00203078

Technical Data
Citations

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.

Solubility for RQ 00203078

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

Preparing Stock Solutions for RQ 00203078

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	1.80 mL	9.01 mL	18.02 mL
5 mM	0.36 mL	1.80 mL	3.60 mL
10 mM	0.18 mL	0.90 mL	1.80 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

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References for RQ 00203078

References are publications that support the biological activity of the product.

Ohmi Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg.Med.Chem.Lett. 2014 PMID: 25455182
Okamoto Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int.J.Oncol. 2012 PMID: 22267123