MDR-652

SKU: orb1305977

Description

MDR-652 is a potent, nonpungent TRPV1 agonist with high affinity (Ki: 11.4 nM hTRPV1) and functional potency (EC50: 5.05 nM hTRPV1). Its strong topical analgesic properties support research in pain pathways, inflammation, and neurobiology, applicable in both in vitro receptor studies and in vivo models of nociception.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1933528-96-1
• MW: 447.95
• Purity: 99.96%
• Formula: C₂₂H₂₃ClFN₃O₂S
• SMILES: CC(C)(C)c1nc(c(CNC(=O)Nc2ccc(CO)c(F)c2)s1)-c1cccc(Cl)c1
• Target: TRP/TRPV Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.16 mM);DMSO:249 mg/mL (555.87 mM)

Bioactivity

• Target 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. 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). 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.).
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

activity, analgesic, MDR 652, MDR652, MDR-652, hTRPV1, ligand, Inhibitor, inhibit, pain, neuropathic, Transient receptor potential channels, TRP Channel, TRPChannel, TRPV Channel, TRPV1, TRPVChannel

Compound Identifiers

PubChem CID

121364823