MDR-652

Alias: MDR-652 MDR652 MDR 652
Cat No.:V2184 Purity: ≥98%
MDR-652 is a novel and highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity.
MDR-652 Chemical Structure CAS No.: 1933528-96-1
Product category: TRP Channel
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

MDR-652 is a novel and highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. agonist discovered to be a strong topical analgesic.

Biological Activity I Assay Protocols (From Reference)
ln Vivo
MDR-652 (0.5 and 5 mg/kg) demonstrated a drop in body temperature that was dose-dependent, corroborating the idea that in intact animals, MDR-652 exhibits TRPV1 agonism [1]. MDR-652 (5–10 mg/kg; intraperitoneal and subcutaneous injection) exhibits 100% maximum potential effect (MPE) in blocking neuropathic pain [1]. Good local pharmacokinetic properties are possessed by MDR-652 [1]. It doesn't seem that MDR-652 is harmful. The LD50 of MDR-652 given intraperitoneally (i.p.) and topically (po) exceeded 200 and 2000 mg/kg, respectively, in single-dose toxicity investigations [1].
Animal Protocol
Animal/Disease Models: ICR mice [1]
Doses: 0.5 and 5 mg/kg
Route of Administration: intraperitonealadministration; 7 hrs (hrs (hours))
Experimental Results: Body temperature diminished in a dose-dependent manner.

Animal/Disease Models: Rat spinal nerve ligation (SNL) model [1]
Doses: 1, 2, 5, 10 mg/kg
Route of Administration: intraperitonealand subcutaneous injection; 24-hour
Experimental Results: intraperitonealadministration demonstrated excellent dosage Dependent analgesic properties, ED50 is 0.5-2 mg/kg. subcutaneous injection also demonstrated excellent analgesic effects, with maximal effects occurring 30 minutes after administration.
References
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H23CLFN3O2S
Molecular Weight
447.95
Exact Mass
447.1184
CAS #
1933528-96-1
SMILES
ClC1=CC=CC(C2=C(CNC(NC3=CC=C(CO)C(F)=C3)=O)SC(C(C)(C)C)=N2)=C1
InChi Key
HKMPJRGWSUCANB-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H23ClFN3O2S/c1-22(2,3)20-27-19(13-5-4-6-15(23)9-13)18(30-20)11-25-21(29)26-16-8-7-14(12-28)17(24)10-16/h4-10,28H,11-12H2,1-3H3,(H2,25,26,29)
Chemical Name
1-((2-(tert-butyl)-4-(3-chlorophenyl)thiazol-5-yl)methyl)-3-(3-fluoro-4-(hydroxymethyl)phenyl)urea
Synonyms
MDR-652 MDR652 MDR 652
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~250 mg/mL (~558.10 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2324 mL 11.1620 mL 22.3239 mL
5 mM 0.4465 mL 2.2324 mL 4.4648 mL
10 mM 0.2232 mL 1.1162 mL 2.2324 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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