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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

Images & Validation

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MDR-652

Key Properties

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CAS Number1933528-96-1
MW447.95
Purity95.04% (May vary between batches)
FormulaC22H23ClFN3O2S
SMILESCC(C)(C)c1nc(c(CNC(=O)Nc2ccc(CO)c(F)c2)s1)-c1cccc(Cl)c1
TargetTRP/TRPV Channel
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.16 mM);DMSO:249 mg/mL (555.87 mM)

Bioactivity

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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

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
121364823 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 mg
$ 100.00
2 mg
$ 130.00
5 mg
$ 180.00
1 ml x 10 mM (in DMSO)
$ 200.00
10 mg
$ 240.00
25 mg
$ 410.00
50 mg
$ 610.00
100 mg
$ 830.00
200 mg
$ 1,120.00
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