| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
FE 999011 can effectively inhibit purified DPP-IV, with an IC50 of 7 nM and a Ki of 2.8 nM[2].
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|---|---|
| ln Vivo |
FE 999011 (1-10 mg/kg; orally; once daily for 7 days; intravenously) dose-dependently reduced blood glucose fluctuations in glucose tolerance tests, inhibited plasma DPP-IV activity for up to 12 hours, and improved insulin sensitivity in male Zucker obese rats after oral administration twice daily for 7 days [1]. FE 999011 (10 mg/kg; orally; twice daily for 26 days) delayed the onset of hyperglycemia in male ZDF rats by 21 days, stabilized food and water intake, reduced hypertriglyceridemia, prevented the increase of free fatty acids, increased basal GLP-1 levels, and upregulated the expression of pancreatic GLP-1 receptors [1].
|
| Animal Protocol |
Animal/Disease Models:Zucker obese rats (male, 8–20 weeks old)[1]
Doses: 1 mg/kg (single oral dose for OGTT pretreatment; single oral dose during OGTT after chronic treatment); 3 mg/kg (single oral dose for OGTT pretreatment; single intravenous injection for IDDGTT pretreatment); 10 mg/kg (single oral dose for acute DPP-IV inhibition; single oral dose for OGTT pretreatment; twice daily for chronic treatment) Route of Administration: Oral; single dose; twice daily for 7 days; intravenous injection; single dose Experimental Results: Plasma DPP-IV activity was inhibited for at least 12 hours, reaching maximum inhibition 1 hour after administration; activity recovered to control levels after 24 hours. The overall glucose response to OGTT decreased in a dose-dependent manner. It reduced blood glucose fluctuations in obese rats to levels comparable to those in lean control rats and enhanced insulin response. Animal/Disease Models:Zucker diabetic obese (ZDF) rats (male, 6 weeks old at the start of the study)[1] Doses: 10 mg/kg (oral once daily; oral twice daily) Route of Administration: Oral; once daily for 26 days; twice daily for 26 days Experimental Results: Not only did it significantly improve blood glucose levels, but it also provided sustained metabolic benefits and enhanced insulin sensitivity. |
| References |
|
| Molecular Formula |
C11H19N3O
|
|---|---|
| Molecular Weight |
209.29
|
| CAS # |
171092-64-1
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC(C)(C)[C@H](N)C(N1[C@@H](CCC1)C#N)=O
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7781 mL | 23.8903 mL | 47.7806 mL | |
| 5 mM | 0.9556 mL | 4.7781 mL | 9.5561 mL | |
| 10 mM | 0.4778 mL | 2.3890 mL | 4.7781 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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