JNJ 17203212

Catalog #: 3361
2 Citations Datasheet / COA / SDS

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JNJ 17203212 | CAS No. 821768-06-3 | TRPV Antagonists

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Description: Reversible, competitive and potent TRPV1 antagonist

Chemical Name: 4-[3-(Trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide

Purity: ≥99%

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Product Details

Citations (2)

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Biological Activity

JNJ 17203212 is a reversible, competitive and potent TRPV1 antagonist (pK_i values are 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively). Inhibits capsaicin- and H⁺-induced channel activation (pIC₅₀ values are 6.32 and 7.23 respectively) and exhibits antitussive and analgesic activity in vivo.

Technical Data

M.Wt:

419.32

Formula:

C₁₇H₁₅F₆N₅O

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

≥99%

Storage:

Store at +4°C

CAS No:

821768-06-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

Dynasore blocks evoked release while augmenting spontaneous synaptic transmission from primary visceral afferents
ME Hofmann, MC Andresen
PLoS ONE, 2017;12(3):e0174915.
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
Swanson et al.
J.Med.Chem., 2005;48:1857
Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain.
Ghilardi et al.
J.Neurosci., 2005;25:3126
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.
Bhattacharya et al.
J.Pharmacol.Exp.Ther., 2007;323:665

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citations for JNJ 17203212

The citations listed below are publications that use Tocris products. Selected citations for JNJ 17203212 include:

2 Citations: Showing 1 - 2

Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain.
Authors: Kelly Et al.
PLoS One 2015;74:252
Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers.
Authors: Vijayvergiya Et al.
PLoS One 2015;10:e0141366

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