Biological Activity
Selective vanilloid receptor antagonist (Ki = 3.2 μM). Inhibits carrageenan inflammation-induced hyperalgesic responses in the rat. Also activates amiloride-sensitive epithelial Na+ channel ENaCδ. Also available as part of the Vanilloid TRPV1 Receptor Tocriset™.
Compound Libraries
Capsazepine is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 376.9 |
| Formula | C19H21ClN2O2S |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 138977-28-3 |
| PubChem ID | 2733484 |
| InChI Key | DRCMAZOSEIMCHM-UHFFFAOYSA-N |
| Smiles | OC1=C(O)C=C2CN(CCCC2=C1)C(=S)NCCC1=CC=C(Cl)C=C1 |
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 | 37.69 | 100 | |
| ethanol | 9.42 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 376.9. 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 | 2.65 mL | 13.27 mL | 26.53 mL |
| 5 mM | 0.53 mL | 2.65 mL | 5.31 mL |
| 10 mM | 0.27 mL | 1.33 mL | 2.65 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Dickenson and Dray (1991) Selective antagonism of capsaicin by capsazepine: evidence for a spinal receptor site in capsaicin-induced antinociception. Br.J.Pharmacol. 104 1045 PMID: 1810591
Kwak et al (1998) A capsaicin-receptor antagonist, capsazepine, reduces inflammation-induced hyperalgesic responses in the rat: evidence for an endogenous capsaicin-like substance. Neuroscience 86 619 PMID: 9881874
Yamamura et al (2004) Capsazepine is a novel activator of the δ subunit of the human epithelial Na+ channel. J.Biol.Chem. 279 44483 PMID: 15308635
Keywords: Capsazepine, supplier, Vanilloid, receptor, antagonists, activators, ENaCdelta, vanilloid, Vanillioid, Receptors, VR1, TRPV, TRP, Channels, Transient, Receptor, Potential, Sodium, Epithelial, ENaC, Na+, TRPV, Epithelial, Sodium, Channels, TRPV, Tocris Bioscience
