| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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Purity: ≥98%
JNJ-17203212 is a novel, potent, reversible, competitive and selective TRPV1 antagonist with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1. JNJ-17203212 inhibits capsaicin- and H+-induced channel activation (pIC50 values are 6.32 and 7.23 respectively) and exhibits antitussive and analgesic activity in vivo. JNJ-17203212, reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. These data indicate that TRPV1 is involved in the pathogenesis of visceral hypersensitivity and that JNJ-17203212 may be a potential therapeutic agent for functional bowel disorders characterized by abdominal hypersensitivity, such as irritable bowel syndrome.
| ln Vitro |
In TRPV1-expressing HEK cells, imperatorin-induced TRPV1 activation (Ca2+ rise) is significantly inhibited by JNJ-17203212 (0.5 μM) [1].
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| ln Vivo |
The early gene c-fos's expression is elevated by inflammatory soup (IS) and is dose-dependently reduced by JNJ-17203212 (0.3 mg/kg; iv) [2]. JNJ-17203212, in a dose-dependent manner, fully inhibits the release of CGRP (neurotransmitter calcitonin gene-related peptide) caused by capsaicin [2].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (260-300 g) [2]
Doses: 0.3 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: The increase in c-fos expression after intracisternal injection of IS was dose-dependent Influence. |
| References |
| Molecular Formula |
C17H15F6N5O
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|---|---|
| Molecular Weight |
419.324323892593
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| Exact Mass |
419.118
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| CAS # |
821768-06-3
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| PubChem CID |
11339118
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.944
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
29
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| Complexity |
564
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JFRYYGVYCWYIDQ-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
1-Piperazinecarboxamide, 4-(3-(trifluoromethyl)-2-pyridinyl)-N-(5-(trifluoromethyl)-2-pyridinyl)-
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| Synonyms |
JNJ-17203212; JNJ 17203212; JNJ17203212.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~238.48 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3848 mL | 11.9241 mL | 23.8481 mL | |
| 5 mM | 0.4770 mL | 2.3848 mL | 4.7696 mL | |
| 10 mM | 0.2385 mL | 1.1924 mL | 2.3848 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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