| Identification | Back Directory | [Name]
1-(2,4-Dichlorophenyl)-N-1-piperidinyl-4-[[(1-pyrrolidinylsulfonyl)amino]methyl]-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-1H-pyrazole-3-carboxamide | [CAS]
1429239-98-4 | [Synonyms]
CB1-IN-1
CB1-IN-4
DBPR 211;DBPR-211
CB1-IN-1(BPRCB1184)
1-(2,4-DICHLOROPHENYL)-N-PIPERIDIN-1-YL-4-[(PYRROLIDIN-1-YLSULFONYLAMINO)METHYL]-5-[5-[2-[4-(TRIFLUOROMETHYL)PHENYL]ETHYNYL]THIOPHEN-2-YL]PYRAZOLE-3-CARBOXAMIDE
1-(2,4-Dichlorophenyl)-N-1-piperidinyl-4-[[(1-pyrrolidinylsulfonyl)amino]methyl]-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-1H-pyrazole-3-carboxamide
1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-N-1-piperidinyl-4-[[(1-pyrrolidinylsulfonyl)amino]methyl]-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]- | [Molecular Formula]
C33H31Cl2F3N6O3S2 | [MOL File]
1429239-98-4.mol | [Molecular Weight]
751.67 |
| Chemical Properties | Back Directory | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 125 mg/mL (166.30 mM) | [form ]
Solid | [pka]
10.21±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively.
IC50 value: 0.3 nM (Ki, CB1R) 21 nM (Ki, CB2R)
Target: CB1R
in vivo: CB1-IN-1 is a novel peripherally restricted cannabinoid 1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice. CB1-IN-1 has great potential to ameliorate this related metabolic syndrome. | [storage]
Store at -20°C | [References]
[1] Chang CP, 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 anta DOI:10.1021/jm401158e |
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