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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C25H26FN5O
- Masse moléculaire:431.51
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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.
-
Cell Line:Murine Min6 pancreatic β-cells
-
Concentration:10 μM
-
Incubation Time:overnight (pre-treatment); 1 h (glucose stimulation)
-
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.
-
Animal Model:C57BL/6J (male, 14 weeks old for OGTT; male, 5-hour fasted for ITT)[1]
-
Dosage:50 mg/kg
-
Administration:i.p.; single dose
-
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.
Chemical Information
-
Masse moléculaire 431.51
-
Formule C25H26FN5O
-
SMILES
O=C(N1CCC2=C(C=CC=C2)C1)C3CCN(C4=NC=CC(NC5=CC=C(C=C5)F)=N4)CC3
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)