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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
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
RQ 00203078 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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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Product Datasheets
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
Do you know of a great paper that uses RQ 00203078 from Tocris? Please let us know.
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Literature in this Area
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Pain Research Product Guide
A collection of over 280 products for pain research, the guide includes research tools for the study of:
- Nociception
- Ion Channels
- G-Protein-Coupled Receptors
- Intracellular Signaling
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.