RQ 00203078
Tocris Bioscience, part of Bio-Techne | Catalog # 5388
Potent and selective TRPM8 antagonist; orally active
Discontinued Product
5388 has been discontinued.
View all TRPM Blockers products.
Key Product Details
Description
Potent and selective TRPM8 antagonist; orally active
Product Description
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.Product Specifications
Molecular Weight
554.85
Formula
C21H13ClF6N2O5S
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for RQ 00203078
For research use only
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