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MDR-652

Catalog No. T22360 CAS 1933528-96-1

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.

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MDR-652, CAS 1933528-96-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 67.00
2 mg	In stock	$ 98.00
5 mg	In stock	$ 163.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 446.00
50 mg	In stock	$ 673.00
100 mg	In stock	$ 958.00
1 mL * 10 mM (in DMSO)	In stock	$ 178.00

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Purity: 99.96%

Biological Description

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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.
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) 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), Sonification is recommended.

References and Literature

1. Jihyae Ann, et al. Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic. J Med Chem. 2020 Jan 9;63(1):418-424.

Related compound libraries

This product is contained In the following compound libraries：

Bioactive Compound Library Covalent Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Ion Channel Inhibitor Library

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Keywords

MDR-652 1933528-96-1 Membrane transporter/Ion channel TRP/TRPV Channel Inhibitor Transient receptor potential channels MDR 652 neuropathic MDR652 analgesic TRP Channel TRPV1 activity pain hTRPV1 inhibit ligand inhibitor

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