A TRPV1 antagonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Capsazepine

Item No. 10007518

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(4-chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide
CAS Number
138977-28-3
Molecular Formula
C19H21ClN2O2S
Formula Weight
376.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2)(1:1): 0.45 mg/mlEthanol: 20 mg/ml
λmax
223, 249, 286 nm
SMILES
OC1=C(O)C=C(CCCN(C(N([H])CCC2=CC=C(Cl)C=C2)=S)C3)C3=C1
InChi Code
InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25)
InChi Key
DRCMAZOSEIMCHM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $36

    Add

    5 mg

    $94

    Add

    10 mg

    $130

    Add

    50 mg

    $523

    Add
    Product Description

    Transient receptor potential vanilloid type 1 (TRPV1) is a member of the transient receptor potential (TRP) family that is activated or sensitized by a variety of endogenous stimuli as a result of tissue injury and inflammation. TRPV1 is upregulated during inflammation and plays a role in the perception of pain.1,2 Capsazepine is a competitive antagonist of transient receptor potential vanilloid type 1 (TRPV1) which blocks the capsaicin-induced uptake of Ca2+ in neonatal rat dorsal root ganglia with an IC50 of 0.42 µM and Chinese hamster ovary cells with an IC50 of 17 nM.1,3 It does not block acid- or heat-induced activation of TRPV1 and may block receptors other than TRPV1.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Doherty, E.M., Fotsch, C., Bo, Y., et al. Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J. Med. Chem. 48(1), 71-90 (2005).

    2. Walker, K.M., Urban, L., Medhurst, S.J., et al. The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain. J. Pharmacol. Exp. Ther. 304(1), 56-60 (2003).

    3. Walpole, S.J., Bevan, S., Bovermann, G., et al. The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin. J. Med. Chem. 37(13), 1942-1954 (1994).

    4. Liu, L., and Simon, S.A. Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia. Neurosci. Lett. 228(1), 29-32 (1997).

    5. Docherty, R.J., Yeats, J.C., and Piper, A.S. Capsazepine block of voltage-activated calcium channels in adult rat dorsal root ganglion neurones in culture. Br. J. Pharmacol. 121(7), 1461-1467 (1997).

    Product Citations

    Owens, R.A., Ignatowska-Jankowska, B., Mustafa, M., et al. Discriminative stimulus properties of the endocannabinoid catabolic enzyme inhibitor SA-57 in mice. J. Pharmacol. Exp. Ther. 358(2), 306-314 (2016).