| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Mavatrep (formerly known as JNJ-39439335) is a novel, orally bioavailable, potent and selective TRPV1 antagonist (Ki = 6.5 nM) with a potential to manage inflammatory pain. It exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6. In a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels, Mavatrep antagonized capsaicin-induced Ca(2+) influx, with an IC50 value of 4.6 nM. In the complete Freund's adjuvant- and carrageenan-induced thermal hypersensitivity models, Mavatrep exhibited full efficacy, with ED80 values of 7.8 and 0.5 mg/kg, respectively, corresponding to plasma levels of 270.8 and 9.2 ng/mL, respectively. On the basis of its superior pharmacologic and safety profile, Mavatrep was selected for clinical development for the treatment of pain.
| ln Vitro |
In HEK293 cells expressing TRPV1 channels, mavatrep (a series of decreasing doses commencing at 1 μM; 25 minutes) suppresses the Ca2+ influx caused by capsaicin [1].
|
|---|---|
| ln Vivo |
Mavatrep (0.1, 0.3, 1, 3, 10 mg/kg; oral; single dosage) exhibits complete reversal of pain in the carrageenan inflammation model and thermal hypersensitivity in the CFA pain inflammation model [1]. In rats, Mavatrep (10 mg/kg; oral; single dosage) shows a notable bioavailability of 51% [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: HEK293 cells (stably expressing TRPV1 channel) Tested Concentrations: A series of decreasing concentrations starting from 1 μM Incubation Duration: 25 minutes Experimental Results: Inhibited capsaicin-induced Ca2+ influx, IC50 value was 4.6 nM. |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (195-350 g; CFA pain inflammation model) [1].
Doses: 10 mg/kg Route of Administration: po (po (oral gavage)) single dose. Experimental Results: Significant reversal of CFA-induced thermal hypersensitivity, which started 30 minutes after administration and lasted for at least 3 hrs (hrs (hours)). Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (195-350 g; CFA pain inflammation model) [1]. Doses: 1, 3, 10, 30 mg/kg Route of Administration: po (po (oral gavage)) single dose. Experimental Results: The thermal hypersensitivity reaction was completely reversed, with ED50 and ED80 values of 1.8 and 7.8 mg/kg, respectively, and corresponding plasma levels of 41.9 and 270.8 ng/mL, respectively. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (195-350 g; carrageenan inflammatory pain model) [1]. Doses: 0.1, 0.3, 1, 3, 10 mg/kg Route of Administration: po (po (oral gavage)) single dose. Experimental Results: The thermal hypersensitivity reaction induced by carrageenan was completely reversed, with ED50 and ED80 values of 0.18 and 0.48 mg/kg, respectively, and the corresponding plasma levels were 3.8 |
| References |
[1]. Parsons W H, 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]-1 H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). Journal of medic
|
| Molecular Formula |
C25H21N2OF3
|
|---|---|
| Molecular Weight |
422.442
|
| CAS # |
956274-94-5
|
| SMILES |
OC(C)(C)C1=CC=CC=C1C2=CC=C3N=C(/C=C/C4=CC=C(C(F)(F)F)C=C4)NC3=C2
|
| InChi Key |
ORDHXXHTBUZRCN-NTEUORMPSA-N
|
| InChi Code |
InChI=1S/C25H21F3N2O/c1-24(2,31)20-6-4-3-5-19(20)17-10-13-21-22(15-17)30-23(29-21)14-9-16-7-11-18(12-8-16)25(26,27)28/h3-15,31H,1-2H3,(H,29,30)/b14-9+
|
| Chemical Name |
(E)-2-(2-(2-(4-(trifluoromethyl)styryl)-1H-benzo[d]imidazol-6-yl)phenyl)propan-2-ol
|
| Synonyms |
JNJ39439335; JNJ 39439335; JNJ-39439335
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~16.67 mg/mL (~39.46 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 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 25.0 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: 2.5 mg/mL (5.92 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3672 mL | 11.8360 mL | 23.6720 mL | |
| 5 mM | 0.4734 mL | 2.3672 mL | 4.7344 mL | |
| 10 mM | 0.2367 mL | 1.1836 mL | 2.3672 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA