A TRPV1 antagonist
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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
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
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    1 mg

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    5 mg

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    10 mg

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    50 mg

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    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).