Mavatrep - CAS 956274-94-5
Catalog number:
956274-94-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C25H21F3N2O
Molecular Weight:
422.44
COA:
Inquire
Targets:
TRP Channel
Description:
Mavatrep is an orally bioavailable, potent and selective TRPV1 antagonist with Ki value of 6.5 nM, which exhibits minimal effect on the enzymatic activity of CYP isoforms 3A4, 1A2, and 2D6. It antagonizes capsaicin-induced Ca2+ influx, with an IC50 value of 4.6 nM in a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels. It blocks the activation of hTRPV1 channels by Capsaicin and pH in a concentration-dependent fashion, with IC50 values of 23 and 6.8 nM respectively. It exhibits superior pharmacodynamic properties in the CFA model of inflammatory pain in vivo. It was selected for clinical development for the treatment of pain. It was developed by Johnson & Johnson and now in clinic phase 1 with no progress.
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Purity:
>98 %
Appearance:
Solid powder
Synonyms:
JNJ-39439335;2-[2-[2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-3H-benzimidazol-5-yl]phenyl]propan-2-ol
Solubility:
DMSO:30mg/mL
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Mavatrep was selected for clinical development for the treatment of pain.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
612.1±65.0 °C | Condition: Press: 760 Torr
Density:
1.300±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
ORDHXXHTBUZRCN-NTEUORMPSA-N
InChI:
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+
Canonical SMILES:
CC(C)(C1=CC=CC=C1C2=CC3=C(C=C2)N=C(N3)C=CC4=CC=C(C=C4)C(F)(F)F)O
Current Developer:
Mavatrep was developed by Johnson & Johnson and now in clinic phase 1 with no progress.
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