RQ 00203078

Cat. No. 5388

RQ 00203078 C21H13ClF6N2O5S [1254205-52-1]

Price and Availability

For RQ 00203078 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid

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.

Technical Data

M.Wt:
554.85
Formula:
C21H13ClF6N2O5S
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1254205-52-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products.

Do you know of a great paper that uses RQ 00203078 from Tocris? If so please let us know.

View Related Products by Target

View Related Products by Product Action

Keywords: RQ 00203078, supplier, RQ00203078, potent, selective, TRPM8, antagonists, transient, receptors, potential, channels, orally, active, melastatin-related, Tocris Bioscience, TRPM Antagonist products

Quick Order

Find multiple products by catalog number

divider line

Pain Research Product Guide

Pain Research Product Guide

Our Pain guide highlights over 280 products for Pain research. Request copy or view PDF today.

divider line

Peripheral Sensitization

Written by Grant D. Nicol and Michael R. Vasko

Pain Life Science Poster

Our Peripheral Sensitization poster gives a summary of the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. Request copy or view PDF today.

divider line

New Products in this Area

AMG 517

Potent TRPV1 antagonist

Sign-up for new product e-alerts
divider line

ISSCR 2017

Win a $1,000 travel grant

ISSCR Travel Grant 2017

Bio-Techne is offering 10 travel grants of $1,000 for ISSCR 2017.