2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Dipeptidyl Peptidase GLP Receptor
  4. 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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FE 999011

FE 999011 Chemical Structure

CAS No. : 171092-64-1

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FE 999011 Related Antibodies

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Description

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[1][2].

In Vitro

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 Related Antibodies
In Vivo

FE 999011 (1-10 mg/kg; p.o.; single dose, twice daily for 7 days; i.v.) dose-dependently reduces glucose excursion during glucose tolerance tests, suppresses plasma DPP-IV activity for up to 12 h, and improves insulin sensitivity after 7 days of twice-daily oral treatment in male Zucker fatty rats[1].
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.

Animal Model: Zucker fatty rats (male, 8-20 weeks of age)[1]
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)
Administration: p.o.; single dose; twice daily for 7 days; i.v.; single dose
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.
Animal Model: Zucker Diabetic Fatty (ZDF) rats (male, 6 weeks of age at study start)[1]
Dosage: 10 mg/kg (once daily p.o.; twice daily p.o.)
Administration: p.o.; once daily for 26 days; twice daily for 26 days
Result: Not only significantly improved blood sugar levels, but it also brought about sustained metabolic benefits and enhances insulin sensitivity.
Molecular Weight

209.29

Formula

C11H19N3O
CAS No.
SMILES

CC(C)(C)[C@H](N)C(N1[C@@H](CCC1)C#N)=O
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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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FE 999011 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:

FE 999011171092-64-1FE999011FE-999011Dipeptidyl PeptidaseGLP ReceptorDPPlipid metabolismrattype 2 diabetes mellitusglucose tolerancehumandipeptidyl peptidase IVGLP-1GLP-1 receptormale ZDF ratsmale Zucker fatty ratsInhibitorinhibitorinhibit

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