FE 999011
FE 999011 is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with IC50 values of 7 nM and 3 nM against human and rat sources, respectively. FE 999011 acts as a glucose tolerance-improving agent and a GLP-1 receptor activator, which reduces blood glucose fluctuation, promotes GLP-1 release and decreases the insulin-glucose ratio. FE 999011 regulates lipid metabolism, delays the onset of diabetes, stabilizes food and water intake, reduces hypertriglyceridemia, prevents the elevation of free fatty acids, and delays the progression of impaired glucose tolerance to disease. FE 999011 can be used in relevant studies of type 2 diabetes.
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- CAS No.: 171092-64-1
- 화학식: C11H19N3O
- 분자량:209.29
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
FE 999011 potently inhibits purified DPP-IV with an IC50 of 7 nM and a Ki of 2.8 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
FE 999011 (10 mg/kg; p.o.; twice daily for 26 days) delays the onset of hyperglycemia by 21 days, stabilizes food and water intake, reduces hypertri-glyceridemia, prevents free fatty acid elevation, increases basal GLP-1 levels, and upregulates pancreatic GLP-1 receptor expression in male ZDF rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zucker fatty rats (male, 8-20 weeks of age)[1]
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Dosage:1 mg/kg (single p.o. for OGTT pretreatment; single p.o. at OGTT after chronic treatment); 3 mg/kg (single p.o. for OGTT pretreatment; single i.v. for IDGTT pretreatment); 10 mg/kg (single p.o. for acute DPP-IV inhibition; single p.o. for OGTT pretreatment; p.o. twice daily for chronic treatment)
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Administration:p.o.; single dose; twice daily for 7 days; i.v.; single dose
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Result:Suppressed plasma DPP-IV activity for at least 12 h, with maximal inhibition at 1 h post-dosing; activity returned to control levels by 24 h.
Produced dose-dependent reductions in integrated glucose response to OGTT.
Reduced glucose excursion in obese rats to match lean control levels, enhanced insulin response.
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Animal Model:Zucker Diabetic Fatty (ZDF) rats (male, 6 weeks of age at study start)[1]
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Dosage:10 mg/kg (once daily p.o.; twice daily p.o.)
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Administration:p.o.; once daily for 26 days; twice daily for 26 days
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Result:Not only significantly improved blood sugar levels, but it also brought about sustained metabolic benefits and enhances insulin sensitivity.
Chemical Information
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CAS No. 171092-64-1
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분자량 209.29
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화학식 C11H19N3O
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SMILES
CC(C)(C)[C@H](N)C(N1[C@@H](CCC1)C#N)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Sudre B, et al. Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male zucker diabetic fatty rats. Diabetes. 2002;51(5):1461-1469. [Content Brief]
[2]. Hunziker D, et al. Inhibitors of dipeptidyl peptidase IV--recent advances and structural views. Curr Top Med Chem. 2005;5(16):1623-1637. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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