SCH 900822
SCH 900822 is a potent and selective glucagon receptor (hGCGR) antagonist that blocks the binding of glucagon to its receptor, thereby reducing hepatic glycogenolysis and gluconeogenesis, thereby lowering blood glucose production. SCH 900822 can be used in the study of type 2 diabetes.
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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: 1220894-09-6
- 分子式: C34H43Cl2N7O2
- 分子量:652.66
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
24 nM
Compound: 1, SCH 900822
|
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
|
[PMID: 24527772] |
| CHO | IC50 |
46 nM
Compound: 1, SCH 900822
|
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
|
[PMID: 24527772] |
| CHO | IC50 |
>10000 nM
Compound: 1, SCH 900822
|
Antagonist activity at human GLP-1R expressed in CHO cells assessed as inhibition of GLP-1-stimulated cAMP production preincubated for 30 mins followed by GLP-1 induction measured after 45 mins by LANCE assay
Antagonist activity at human GLP-1R expressed in CHO cells assessed as inhibition of GLP-1-stimulated cAMP production preincubated for 30 mins followed by GLP-1 induction measured after 45 mins by LANCE assay
|
[PMID: 24527772] |
化学情報
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CAS 番号 1220894-09-6
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分子量 652.66
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分子式 C34H43Cl2N7O2
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SMILES
O=C(C1=CC=C([C@@H](CCC(C)(C)C)N([C@]2(N=C3C4=CC(Cl)=CC(Cl)=C4)CC[C@@H](C(C)(C)C)CC2)C3=O)C=C1)NCC5=NN=NN5
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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.
純度とドキュメンテーション
参考文献
[1]. DeMong D, et al. The Discovery of N-((2 H-Tetrazol-5-yl) methyl)-4-((R)-1-((5 r, 8 R)-8-(tert-butyl)-3-(3, 5-dichlorophenyl)-2-oxo-1, 4-diazaspiro [4.5] dec-3-en-1-yl)-4, 4-dimethylpentyl) benzamide (SCH 900822): A Potent and Selective Glucagon Receptor Antagonist[J]. Journal of medicinal chemistry, 2014, 57(6): 2601-2610. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)