A CB1 receptor inverse agonist
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BPR0912

Item No. 10678

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(2,4-dichlorophenyl)-4-ethyl-N-1-piperidinyl-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-1H-pyrazole-3-carboxamide
CAS Number
1253641-65-4
Synonyms
  • TM38837
Molecular Formula
C30H25Cl2F3N4OS
Formula Weight
617.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CCC1=C(C2=CC=C(C#CC3=CC=C(C(F)(F)F)C=C3)S2)N(C4=CC=C(Cl)C=C4Cl)N=C1C(NN5CCCCC5)=O
InChi Code
InChI=1S/C30H25Cl2F3N4OS/c1-2-23-27(29(40)37-38-16-4-3-5-17-38)36-39(25-14-11-21(31)18-24(25)32)28(23)26-15-13-22(41-26)12-8-19-6-9-20(10-7-19)30(33,34)35/h6-7,9-11,13-15,18H,2-5,16-17H2,1H3,(H,37,40)
InChi Key
VQOCBFYUDSBDCZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    BPR0912 is a cannabinoid 1 (CB1) receptor inverse agonist (IC50 = 8.5 nM for the human receptor).1 It is selective for CB1 over CB2 receptors (IC50 = 604.9 nM for the human receptor). In vivo, BPR0912 (10 mg/kg per day) inhibits diet-induced increases in body weight, epididymal and inguinal fat pad mass, and serum levels of insulin and triglycerides, as well as hepatic triglyceride levels, in a mouse model of high-fat diet-induced obesity.2 It also increases the levels of mitochondrial uncoupling protein 1 (Ucp1) in brown adipose tissue from, as well as induces thermogenesis in, mice in the same mouse model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hung, M.-S., Chang, C.-P., Li, T.-C., et al. Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist. ChemMedChem 5(9), 1439-1443 (2010).

    2. Hsiao, W.C., Shia, K.S., Wang, Y.T., et al. A novel peripheral cannabinoid receptor 1 antagonist, BPR0912, reduces weight independently of food intake and modulates thermogenesis. Diabetes Obes. Metab. 17(5), 495-504 (2015).