2. Protein Tyrosine Kinase/RTK
  3. Insulin Receptor
  4. 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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BDM71230

BDM71230 Chemical Structure

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BDM71230 Related Antibodies

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Description

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[1].

In Vitro

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.

BDM71230 Related Antibodies

ELISA Assay[1]

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.
Parmacokinetics
Species Dose Route Cmax T1/2
Mice[1] 30 mg/kg i.p. 5.3 μg/mL 81 min
In Vivo

BDM71230 (50 mg/kg; i.p.; single dose) significantly increases glucose intolerance in mice during an oral glucose tolerance test and slightly blunts insulin's glucose-lowering effect during an insulin tolerance test[1].

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.
Molecular Weight

431.51

Formula

C25H26FN5O
SMILES

O=C(N1CCC2=C(C=CC=C2)C1)C3CCN(C4=NC=CC(NC5=CC=C(C=C5)F)=N4)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BDM71230 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BDM71230BDM 71230BDM-71230Insulin ReceptorInsulin-Degrading Enzymeinsulin hydrolysisinsulin tolerance testoral glucose tolerance testmouse plasmaglucose intoleranceMin6 murine pancreatic β-cellsIDE dimer interfaceInhibitorinhibitorinhibit

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