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MDR-652

Name: MDR-652
Brand: TargetMol
SKU: T22360
Price: 58 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22360Cas No. 1933528-96-1

MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1), with Ki values of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively, and EC50s of 5.05 nM and 93 nM for hTRPV1 and rTRPV1, respectively. MDR-652 is a potent topical analgesic.

MDR-652

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Purity: 99.96%

Catalog No. T22360Cas No. 1933528-96-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$58	In Stock	In Stock
2 mg	$84	In Stock	In Stock
5 mg	$139	In Stock	In Stock
10 mg	$198	In Stock	In Stock
25 mg	$368	In Stock	In Stock
50 mg	$569	In Stock	In Stock
100 mg	$786	In Stock	In Stock
200 mg	$1,080	-	In Stock
1 mL x 10 mM (in DMSO)	$153	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.96%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1), with Ki values of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively, and EC50s of 5.05 nM and 93 nM for hTRPV1 and rTRPV1, respectively. MDR-652 is a potent topical analgesic.
Targets&IC50	TRPV1 (human):11.4 nM (Ki), TRPV1 (human):5.05 nM (EC50), TRPV1 (rat):23.8 nM (Ki), TRPV1 (rat):93 nM (EC50)
In vivo	MDR-652 (0.5 and 5 mg/kg) demonstrates a dose-dependent decrease in body temperature, indicating TRPV1 agonism in intact animals[1]. It exhibits potent analgesic activity in neuropathic pain models and blocks capsaicin-induced allodynia, with dermal accumulation and minimal transdermal absorption. At 5-10 mg/kg (i.p. and s.c.), MDR-652 completely inhibits neuropathic pain, achieving 100% maximum possible effect (MPE)[1]. MDR-652 has a promising topical pharmacokinetic profile, shows weak systemic toxicity, and is negative in genotoxicity assays. In a single-dose toxicity study, the LD50 of MDR-652 exceeds 200 mg/kg (i.p.) and 2000 mg/kg (p.o.)[1].
Animal Research	MDR-652 (0.5 and 5 mg/kg; Administered intraperitoneally; 7 hours; ICR mouse) decreased body temperature in a dose-dependent manner. MDR-652 (1, 2, 5, and 10 mg/kg; Administered intraperitoneally and subcutaneously; 24 hours; Rats with spinal nerve ligation (SNL) model)The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED50 of 0.5-2 mg/kg. The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration.

Chemical Properties

Molecular Weight	447.95
Formula	C₂₂H₂₃ClFN₃O₂S
Cas No.	1933528-96-1
Smiles	CC(C)(C)c1nc(c(CNC(=O)Nc2ccc(CO)c(F)c2)s1)-c1cccc(Cl)c1
Relative Density.	1.330 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 249 mg/mL (555.87 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.16 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2324 mL	11.1620 mL	22.3239 mL	111.6196 mL
5 mM	0.4465 mL	2.2324 mL	4.4648 mL	22.3239 mL
10 mM	0.2232 mL	1.1162 mL	2.2324 mL	11.1620 mL
20 mM	0.1116 mL	0.5581 mL	1.1162 mL	5.5810 mL
50 mM	0.0446 mL	0.2232 mL	0.4465 mL	2.2324 mL
100 mM	0.0223 mL	0.1116 mL	0.2232 mL	1.1162 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc