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

Mavatrep  (Synonyms: JNJ-39439335)

Cat. No.: HY-16935 Purity: 99.60%
COA Handling Instructions

Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain.

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 275 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 275 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
Estimated Time of Arrival: December 31
25 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1360 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2200 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

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

View All Isoforms
TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain[1].

In Vitro

Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca2+ influx in HEK293 cells expressing TRPV1 channels[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HEK293 cells (stably expressing TRPV1 channels)
Concentration: Series of decreasing concentrations from 1 μM
Incubation Time: 25 min
Result: Inhibited capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM.
In Vivo

Mavatrep (1, 3, 10, 30 mg/kg; p.o.; single) shows complete reversal of thermal hypersensitivity both in CFA model of inflammatory of pain and (0.1, 0.3, 1, 3, 10 mg/kg) carrageenan model of inflammatory pain[1].
Mavatrep (10 mg/kg; p.o.; single) exhibits substantial bioavailability in the rat (51%)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain)[1].
Dosage: 10 mg/kg
Administration: Oral administration, single.
Result: Significantly reversed CFA-induced thermal hypersensitivity, beginning 30 min after administration and lasting for at least 3 h.
Animal Model: Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain)[1].
Dosage: 1, 3, 10, 30 mg/kg
Administration: Oral administration, single.
Result: Exhibited complete reversal of thermal hypersensitivity, with ED50 and ED80 values of 1.8 and 7.8 mg/kg, and the corresponding plasma levels were 41.9 and 270.8 ng/mL, respectively.
Animal Model: Male Sprague-Dawley rats (195-350 g; carrageenan model of inflammatory pain)[1].
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: Oral administration, single.
Result: Completely reversed carrageenan-induced thermal hypersensitivity, with ED50 and ED80 values of 0.18 and 0.48 mg/kg, and the corresponding plasma levels were 3.8 and 9.2 ng/mL, respectively.
Animal Model: Male Sprague-Dawley rats (195-350 g)[1].
Dosage: 2 mg/kg (for i.v.); 10 mg/kg (for p.o.). (Dissolved in 20% HPβCD)
Administration: Oral administration, single.
Result: 1.19 Pharmacokinetic Parameters of Mavatrep in male Sprague-Dawley rats[1].
IV (2 mg/kg) PO (10 mg/kg)
CL (mL/min/kg) Vss (L/kg) T1/2 (h) Cmax (ng/mL) AUCmax (ng•h/mL) T1/2 (h) F (%)
33 10 3.4 421 4203 3.8 51
Clinical Trial
Molecular Weight

422.44

Appearance

Solid

Formula

C25H21F3N2O
CAS No.
SMILES

OC(C)(C)C1=CC=CC=C1C2=CC=C3N=C(/C=C/C4=CC=C(C(F)(F)F)C=C4)NC3=C2
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 : 16.67 mg/mL (39.46 mM; ultrasonic and warming and heat to 60°C)

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 available by MCE.
Purity & Documentation

Purity: 99.60%

COA (246 KB) HNMR (266 KB) LCMS (261 KB)

Handling Instructions (2659 KB)
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Mavatrep956274-94-5JNJ-39439335JNJ39439335JNJ 39439335TRP ChannelTransient receptor potential channelsneuropathic painHEK293capsaicincalcium ionshTRPV1 channelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Mavatrep
Cat. No.:
HY-16935
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email address *

Phone number

 

Department *

Organization name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.