BPR-890
BPR-890 is a potent agonist of CB1. BPR-890 exhibits excellent CB2/1 selectivity and has in vivo efficacy in diet-induced obese mouse model.
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- CAS No.: 1170700-86-3
- Formule: C23H21Cl3N4S
- Masse moléculaire:491.86
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
5.1 nM
Compound: 24, BPR-890
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Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding
Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding
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[PMID: 19530697] |
| HEK293 | IC50 |
12 nM
Compound: 24, BPR-890
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Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells
Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells
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[PMID: 19530697] |
| HEK293 | IC50 |
4746 nM
Compound: 24, BPR-890
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Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells
Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells
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[PMID: 19530697] |
Chemical Information
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CAS No. 1170700-86-3
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Masse moléculaire 491.86
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Formule C23H21Cl3N4S
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SMILES
S=C1N=C(C2=NN(C3=CC=C(Cl)C=C3Cl)C(C4=CC=C(Cl)C=C4)=C2CC)N(C)C1(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Wu, C. H., et al., (2009). Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice. Journal of medicinal chemistry, 52(14), 4496-4510. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BPR-890 Related Classifications
HY-14140 Related Classifications
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