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CB1-IN-1(BPRCB1184)

  Cat. No.:  DC7790   Featured
Chemical Structure
1429239-98-4
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1429239-98-4
Synonyms: DBPR 211,DBPR-211;DBPR211
SMILES: C1CCN(CC1)NC(=O)C2=NN(C(=C2CNS(=O)(=O)N3CCCC3)C4=CC=C(S4)C#CC5=CC=C(C=C5)C(F)(F)F)C6=C(C=C(C=C6)Cl)Cl
Formula: C33H31Cl2F3N6O3S2
M.Wt: 750.12
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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 antagonist with significant weight-loss efficacy in diet-induced obese mice. J Med Chem. 2013 Dec 27;56(24):9920-9933.
Description: CB1-IN-1 is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively.
Target: 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.
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
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC28290 TM38837 TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.
DC8876 Rimonabant(SR141716) Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
DC9383 Rimonabant (Hydrochloride) Rimonabant Hcl(SR141716A) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
DC11330 LY320135 LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).
DC7790 CB1-IN-1(BPRCB1184) 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.
DC8765 AM251 AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).
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