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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 |
Description | MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1) with Ki value of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1 respectively and EC50s for hTRPV1 and rTRPV1 are 5.05 and 93 nM respectively. MDR-652 is a potent topical analgesic. |
In vivo | MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal[1]. Potent analgesic activity was observed in models of neuropathic pain, and MDR-652 blocked capsaicin induced allodynia, showing dermal accumulation with little transdermal absorption. MDR-652 (5-10 mg/kg; i.p. and s.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) [1]. MDR-652 has a promising topical pharmacokinetic profile[1]. MDR-652 displays weak systemic toxicity and is negative in assays of genotoxicity. In a single-dose toxicity study, the LD50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively[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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 249 mg/mL (555.86 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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