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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- CAS No.: 1220894-09-6
- Formule: C34H43Cl2N7O2
- Masse moléculaire:652.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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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] |
Chemical Information
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CAS No. 1220894-09-6
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Masse moléculaire 652.66
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Formule 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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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]. 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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)