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DBPR211
- Soluble in DMSO
- MF: C33H31Cl2F3N6O3S2
- MW: 751.67
Description
DBPR211 is a potent, selective and peripherally restricted cannabinoid CB1 receptor antagonist/inverse agonist with a reported Ki value of 0.3 nM. Its limited central nervous system exposure is intended to separate peripheral CB1-dependent metabolic effects from the behavioral and psychiatric effects associated with brain-penetrant CB1 inverse agonists.
DBPR211 reduced body weight in diet-induced obese mice and is used to examine the contribution of peripheral CB1 signaling to appetite-independent metabolic regulation, adipose and hepatic lipid metabolism, insulin sensitivity and cardiometabolic disease. Brain-penetration and receptor-occupancy controls remain important when interpreting in vivo effects.
Key Features
- High-affinity CB1 receptor antagonist/inverse agonist
- Ki: 0.3 nM
- Designed for peripheral restriction
- Reduces body weight in diet-induced obesity models
Applications
- Peripheral CB1 receptor pharmacology
- Obesity and metabolic-disease models
- Hepatic and adipose lipid metabolism studies
- CNS versus peripheral cannabinoid signaling research
More Information
| Parent CAS No. | 1429239-98-4 |
|---|---|
| Chemical Name | 1-(2,4-Dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-1H-pyrazole-3-carboxamide |
| SMILES | C1(N2C(C3SC(C#CC4C=CC(C(F)(F)F)=CC=4)=CC=3)=C(CNS(N3CCCC3)(=O)=O)C(C(=O)NN3CCCCC3)=N2)C(Cl)=CC(Cl)=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C33H31Cl2F3N6O3S2/c34-24-11-14-28(27(35)20-24)44-31(29-15-13-25(48-29)12-8-22-6-9-23(10-7-22)33(36,37)38)26(21-39-49(46,47)43-18-4-5-19-43)30(40-44)32(45)41-42-16-2-1-3-17-42/h6-7,9-11,13-15,20,39H,1-5,16-19,21H2,(H,41,45) |
| InChiKey | KAIYFJUWIBTYPK-UHFFFAOYSA-N |
| CID | 71515460 |
| Short Description | CB1 antagonist |
References
- CP Chang et al. Fluorine-18 isotope labeling for positron emission tomography imaging. Direct evidence for DBPR211 as a peripherally restricted CB1 inverse agonist. Bioorg Med Chem. 2019 Jan 1;27(1):216-223.
- CP Chang et al. Discovery of 1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice. J Med Chem. 2013 Dec 27;56(24):9920-33.
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