| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 4-[[3-chloro-5-(trifluoromethyl)pyridin-2-yl]-[[4-(trifluoromethoxy)phenyl]methyl]sulfamoyl]benzoic acid.
- CAS number: 1254205-52-1
- Molecular formula: C21H13ClF6N2O5S.
- Purity: >99%
- Concentration: 1 nM - 1 µM.
- Form: Lyophilized powder.
- Solubility: Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
- Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: TRPM8 channel
- Source: Synthetic
- Activity: RQ 00203078 is a potent and selective TRPM8 antagonist, shown to inhibit menthol-evoked human and rat TRPM8-mediated calcium influx with IC50 of 8.3 nM and 5.8 nM, respectively, while being highly selective over hTRPV4, h/rTRPV1, h/rTRPA1 and TRPM21,2.
Scientific background
RQ 00203078 is a synthetic compound that acts as a potent and highly selective TRPM8 channel blocker with IC50 values of 8.3 nM and 5.8 nM for human and rat TRPM8 respectively. The compound shows very little inhibitory action against TRPV1, TRPA1, TRPV4 and TRPM2 channel. It is orally available and may be a useful tool for assessing the potential therapeutic use of TRPM81,2.TRPM8 is a Ca2+-permeable, nonselective cation channel that is activated by temperatures in the range of 8-28°C and by chemical agonists such as menthol and icilin. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons. TRPM8 gene is up-regulated in prostate cancer and other malignancies1,3.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
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