Mavatrep, aslo known as JNJ-39439335, is a potent and selective TRPV1 antagonist. . 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.
MedKoo Cat#: 319674
Name: Mavatrep
CAS#: 956274-94-5
Chemical Formula: C25H21F3N2O
Exact Mass: 422.1606
Molecular Weight: 422.45
Elemental Analysis: C, 71.08; H, 5.01; F, 13.49; N, 6.63; O, 3.79
The following data is based on the product molecular weight 422.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
