BDM71230
BDM71230 is an orally active inducer of insulin-degrading enzyme (IDE), with an EC50 of 1.9 μM against human IDE. BDM71230 binds to the interface of IDE dimers and enhances the catalytic activity of IDE via steric effects. BDM71230 can potentiate the hydrolytic effect of IDE on insulin and slightly attenuate the hypoglycemic effect of insulin. BDM71230 serves as a pharmacological tool for investigating IDE function and is applicable to studies related to glucose intolerance.
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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。
- 分子式: C25H26FN5O
- 分子量:431.51
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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
BDM71230 (1.9-100 μM) potently activates recombinant human IDE catalytic activity with an EC50 of 1.9 μM and a 4.1-fold maximum activation at 100 μM[1].
BDM71230 (10 μM; overnight pre-treatment, 1 h glucose stimulation) significantly reduces glucose-stimulated insulin secretion in Min6 murine pancreatic β-cells across low, medium, and high glucose concentrations[1].
BDM71230 (10 μM; up to 24 h) is highly stable in mouse plasma with a half-life exceeding 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine Min6 pancreatic β-cells
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Concentration:10 μM
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Incubation Time:overnight (pre-treatment); 1 h (glucose stimulation)
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Result:Significantly decreased secreted insulin levels in Min6 cells stimulated with 2.8 mM, 11 mM, or 20 mM glucose.
| Species | Dose | Route | Cmax | T1/2 |
|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 5.3 μg/mL | 81 min |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 14 weeks old for OGTT; male, 5-hour fasted for ITT)[1]
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Dosage:50 mg/kg
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Administration:i.p.; single dose
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Result:Significantly increased blood glucose levels at 45, 75, and 105 minutes post-glucose challenge during OGTT compared to vehicle.
Slightly decreased the glucose-lowering effect of insulin at 30 minutes post-insulin injection during ITT.
化学情報
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分子量 431.51
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分子式 C25H26FN5O
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SMILES
O=C(N1CCC2=C(C=CC=C2)C1)C3CCN(C4=NC=CC(NC5=CC=C(C=C5)F)=N4)CC3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)