Biological Activity
TRPV1 positive allosteric modulator. Potentiates vanilloid and proton activation of TRPV1 channels. Exhibits analgesic effects in combination with capsaicin (Cat. No. 0462) in rats. Also prolongs capsaicin-induced hypothermia in mice.
Technical Data
| M. Wt | 389.51 |
| Formula | C21H27NO4S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 212200-21-0 |
| PubChem ID | 9843337 |
| InChI Key | DMVMFYWYJCPZGS-UHFFFAOYSA-N |
| Smiles | CCC1C(C(OCC)=O)=C(C2=CC=CC=C2)NC(C)=C1C(SCCOC)=O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.95 | 100 | |
| ethanol | 19.48 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 389.51. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.57 mL | 12.84 mL | 25.67 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.13 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kaszas et al (2012) Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. J.Pharmacol.Exp.Ther. 340 152 PMID: 22005042
Lebovitz et al (2012) Positive allosteric modulation of TRPV1 as a novel analgesic mechanism. Mol.Pain 8 PMID: 22998799
Roh et al (2008) Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1). Bioorg.Med.Chem. 16 9349 PMID: 18809334
Keywords: MRS 1477, supplier, MRS1477, TRPV1, transient, receptors, potential, channels, positive, allosteric, modulators, analgesic, TRPV, TRPV, Tocris Bioscience
