1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. Mavatrep

Mavatrep (Synonyms: JNJ-39439335)

Cat. No.: HY-16935 Purity: 99.85%
Handling Instructions

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.

For research use only. We do not sell to patients.

Mavatrep Chemical Structure

Mavatrep Chemical Structure

CAS No. : 956274-94-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 462 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6. IC50 value: 6.5 nM (Ki, for TRPV1) Target: TRPV1 in vitro: Mavatrep exhibits superior pharmacodynamic properties. In a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels, Mavatrep antagonizes capsaicin-induced Ca2+ influx, with an IC50 value of 4.6 nM. Mavatrep blocks the activation of hTRPV1 channels by Capsaicin (1 μM) and by pH (5.0) in a concentration-dependent fashion, with IC50 values of 23 and 6.8 nM, respectively. in vivo: Mavatrep exhibits superior pharmacodynamic properties in the CFA model of inflammatory pain.

Clinical Trial
Molecular Weight

422.44

Formula

C₂₅H₂₁F₃N₂O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (66.28 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.92 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Product Name:
Mavatrep
Cat. No.:
HY-16935
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