Mavatrep (Synonyms: JNJ-39439335)

Name: Mavatrep
Brand: MedChemExpress
SKU: HY-16935
Rating: 4.5 (1 reviews)

Cat. No.: HY-16935 Purity: 99.60%: FAQs
Data Sheet SDS COA Handling Instructions

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Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (K_i=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

CAS No. : 956274-94-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 198	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 198	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 830	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	21 nM Compound: 4, Mavatrep	Antagonist activity at recombinant rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge Antagonist activity at recombinant rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge	[PMID: 25850459]
HEK293	IC₅₀	23 nM Compound: 4, Mavatrep	Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced current measured for 150 secs by patch clamp assay Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced current measured for 150 secs by patch clamp assay	[PMID: 25850459]
HEK293	IC₅₀	4.6 nM Compound: 4, Mavatrep	Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge	[PMID: 25850459]
HEK293	IC₅₀	6.8 nM Compound: 4, Mavatrep	Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of pH 5-induced current measured for 150 secs by patch clamp assay Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of pH 5-induced current measured for 150 secs by patch clamp assay	[PMID: 25850459]

In Vitro

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

MedChemExpress (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].

MedChemExpress (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)	V_ss (L/kg)	T_1/2 (h)		C_max (ng/mL)	AUC_max (ng•h/mL)	T_1/2 (h)	F (%)
33	10	3.4		421	4203	3.8	51

Clinical Trial

Molecular Weight

422.44

Formula

C₂₅H₂₁F₃N₂O

CAS No.

956274-94-5

Appearance

Solid

Color

White to off-white

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL (39.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.60%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

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

Handling Instructions (2659 KB)

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3672 mL	11.8360 mL	23.6720 mL	59.1800 mL
	5 mM	0.4734 mL	2.3672 mL	4.7344 mL	11.8360 mL
	10 mM	0.2367 mL	1.1836 mL	2.3672 mL	5.9180 mL
	15 mM	0.1578 mL	0.7891 mL	1.5781 mL	3.9453 mL
	20 mM	0.1184 mL	0.5918 mL	1.1836 mL	2.9590 mL
	25 mM	0.0947 mL	0.4734 mL	0.9469 mL	2.3672 mL
	30 mM	0.0789 mL	0.3945 mL	0.7891 mL	1.9727 mL

Mavatrep Related Classifications

Neurological Disease

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.

Keywords:

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

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Mavatrep (Synonyms: JNJ-39439335)

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Complete Stock Solution Preparation Table

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