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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1170700-86-3
- 分子式: C23H21Cl3N4S
- 分子量:491.86
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
5.1 nM
Compound: 24, BPR-890
|
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
|
[PMID: 19530697] |
| HEK293 | IC50 |
12 nM
Compound: 24, BPR-890
|
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
|
[PMID: 19530697] |
| HEK293 | IC50 |
4746 nM
Compound: 24, BPR-890
|
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
|
[PMID: 19530697] |
化学情報
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CAS 番号 1170700-86-3
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分子量 491.86
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)