JNJ 17203212 |
| رقم الكتالوجGC15427 |
JNJ 17203212 هو خصم TRPV1 انتقائي وقوي وتنافسي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 821768-06-3
Sample solution is provided at 25 µL, 10mM.
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JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.IC50 value: 65 nM (human TRPV1), 102 nM (rat TRPV1)Target: TRPVin vivo: JNJ-17203212 reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. Throughout this study, colonic sensitivity was assessed via quantification of VMR to CRD in rats following a single, oral administration of JNJ-17203212 (3, 10 or 30 mg/kg) or vehicle. [1] Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents core hypothermia evoked by sc capsaicin. Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents capsaicin-evoked hypothermia in a dose-response manner. [2]
References:
[1]. Wiskur BJ, et al. A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats. Methods Find Exp Clin Pharmacol. 2010 Oct;32(8):557-64.
[2]. Swanson DM, et al. 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. J Med Chem. 2005 Mar 24;48(6):185
| Cas No. | 821768-06-3 | SDF | |
| Chemical Name | 4-(3-(trifluoromethyl)pyridin-2-yl)-N-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-carboxamide | ||
| Canonical SMILES | FC(F)(C1=CC=CN=C1N2CCN(C(NC3=NC=C(C(F)(F)F)C=C3)=O)CC2)F | ||
| Formula | C17H15F6N5O | M.Wt | 419.32 |
| الذوبان | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3848 mL | 11.9241 mL | 23.8481 mL |
| 5 mM | 0.477 mL | 2.3848 mL | 4.7696 mL |
| 10 mM | 0.2385 mL | 1.1924 mL | 2.3848 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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