Mavatrep (Synonyms: JNJ-39439335) |
رقم الكتالوجGC14761
One-Click Copy Product Info
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Mavatrep (JNJ-39439335) هو مضاد TRPV1 نشط عن طريق الفم وانتقائي وقوي مع تقارب كبير لقنوات hTRPV1 (Ki = 6.5 نانومتر)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 956274-94-5
Sample solution is provided at 25 µL, 10mM.
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Mavatrep is a potent and orally bioavailable antagonist of TRPV1 with IC50 value of 4.6 nM [1][2].
Transient receptor potential vanilloid-1 (TRPV1) is a thermosensitive and nonselective cation channel, and is a member of the TRP channel superfamily. The channel is activated by acidic pH (<6.8), thermal stimuli (>43℃), and endogenous lipidic mediators (anandamide and oxidative metabolites of linoleic acid) [1].
Mavatrep is a potent and orally bioavailable TRPV1 antagonist. In HEK293 cells that stably express human or rat TRPV1 (rTRPV1) channels, mavatrep (1 μM) inhibited capsaicin-induced Ca2+ influx with IC50 values of 4.6 nM and 21 nM. In whole-cell patch clamp electrophysiology assay, mavatrep concentration-dependently inhibited the activation of hTRPV1 channels by pH (5.0) and capsaicin (1 μM) with IC50 values of 6.8 and 23 nM, respectively. Mavatrep (0.1 μM) also inhibited 74 ± 8.1% heat-evoked currents mediated by hTRPV1 [1].
In the CFA model of inflammatory of pain, mavatrep (10 mg/kg po) significantly reversed CFA-induced thermal hypersensitivity with ED50 and ED80 values of 1.8 and 7.8 mg/kg, respectively [1].
Reference:
[1]. Parsons WH, Calvo RR, Cheung W, et al. Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem, 2015, 58(9): 3859-3874.
| Cas No. | 956274-94-5 | SDF | |
| المرادفات | JNJ-39439335 | ||
| Chemical Name | (E)-2-(2-(2-(4-(trifluoromethyl)styryl)-1H-benzo[d]imidazol-6-yl)phenyl)propan-2-ol | ||
| Canonical SMILES | CC(C1=CC=CC=C1C2=CC(N3)=C(N=C3/C([H])=C([H])/C4=CC=C(C(F)(F)F)C=C4)C=C2)(O)C | ||
| Formula | C25H21F3N2O | M.Wt | 422.44 |
| الذوبان | DMSO : 16.67 mg/mL (39.46 mM; ultrasonic and warming and heat to 60°C) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3672 mL | 11.836 mL | 23.672 mL |
| 5 mM | 473.4 μL | 2.3672 mL | 4.7344 mL |
| 10 mM | 236.7 μL | 1.1836 mL | 2.3672 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)