CB1-IN-4 ( DBPR211; DBPR 211; DBPR-211; CB1-IN-1 )

Catalog No. M11811 CAS No. 1429239-98-4

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Product Name

CB1-IN-4
Note

Research use only, not for human use.
Brief Description

CB1-IN-4 is a potent, selective, peripherally restricted cannabinoid-1 (CB1) receptor antagonist with Ki of 0.3 nM, EC50 of 3.0 nM.
Description

CB1-IN-4 is a potent, selective, peripherally restricted cannabinoid-1 (CB1) receptor antagonist with Ki of 0.3 nM, EC50 of 3.0 nM; possess a low probability to cross BBB as a peripherally restricted CB1R antagonist, exhibits significant weight-loss efficacy in DIO mice, also displays 163 clean off-target profiles and potential for treating obesity and the related metabolic syndrome.
Synonyms

DBPR211; DBPR 211; DBPR-211; CB1-IN-1
Pathway

GPCR/G Protein
Target

Cannabinoid Receptor
Recptor

Cannabinoid Receptor
Research Area

Neurological Disease
Indication

——

CAS Number

1429239-98-4
Formula Weight

751.67
Molecular Formula

C33H31Cl2F3N6O3S2
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(C#CC4=CC=C(C(F)(F)F)C=C4)S3)=C1CNS(=O)(N5CCCC5)=O)NN6CCCCC6
Chemical Name

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]-

1. Chang CP, et al. J Med Chem. 2013 Dec 27;56(24):9920-33.

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