A TRPV1 antagonist
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JNJ-17203212

Item No. 30930

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide
CAS Number
821768-06-3
Molecular Formula
C17H15F6N5O
Formula Weight
419.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/ml
λmax
249 nm
SMILES
FC(F)(F)C1=CC=C(NC(N2CCN(C3=NC=CC=C3C(F)(F)F)CC2)=O)N=C1
InChi Code
InChI=1S/C17H15F6N5O/c18-16(19,20)11-3-4-13(25-10-11)26-15(29)28-8-6-27(7-9-28)14-12(17(21,22)23)2-1-5-24-14/h1-5,10H,6-9H2,(H,25,26,29)
InChi Key
JFRYYGVYCWYIDQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $129

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    10 mg

    $194

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    25 mg

    $351

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    50 mg

    $574

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    Product Description

    JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).1 It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.2 JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bhattacharya, A., Scott, B.P., Nasser, N., et al. Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J. Pharmacol. Exp. Ther. 323(2), 665-674 (2007).

    2. Ghilardi, J.R., Röhrich, H., Lindsay, T.H., et al. Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J. Neurosci. 25(12), 3126-3131 (2005).

    3. Meents, J.E., Hoffmann, J., Chaplan, S.R., et al. Two TRPV1 receptor antagonists are effective in two different experimental models of migraine. J. Headache Pain 16, 57 (2015).