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MDR-652
🥰Excellent
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
🥰Excellent
Purity: 99.96%
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $67 | In Stock | |
| 2 mg | $98 | In Stock | |
| 5 mg | $163 | In Stock | |
| 10 mg | $247 | In Stock | |
| 25 mg | $446 | In Stock | |
| 50 mg | $673 | In Stock | |
| 100 mg | $958 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $178 | In Stock |
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Purity:99.96%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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 (rat):23.8 nM (Ki), TRPV1 (rat):93 nM (EC50), TRPV1 (human):11.4 nM (Ki), TRPV1 (human):5.05 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. |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 249 mg/mL (555.86 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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