DBPR108
Based on 1 publication(s) in Google Scholar
DBPR108 is an orally active, selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 of 15 nM. DBPR108 reduces glycated hemoglobin, fasting plasma glucose and postprandial plasma glucose levels, increases serum active GLP-1 and insulin levels, and improves glucose tolerance. DBPR108 can be used in research related to type 2 diabetes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.93%
- No. CAS: 1186426-66-3
- Fòrmula: C16H25FN4O2
- Peso molecular:324.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DBPR108
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Actividad biológica
Descripciòn
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DPP-4 15 nM (IC50) |
GLP-1 |
In Vitro
DBPR108 potently and selectively inhibits DPP-4 with an IC50 of 15 nM, and exhibits no significant inhibitory activity against DPP-8, DPP-9 or fibroblast activation protein (IC50 >50 μM)[1].
The IC50 values of DBPR108 against DPP-4 in human, rodent, canine and monkey plasma range from 4.1 to 20.4 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | AUC0-∞ | T1/2 |
|---|---|---|---|---|---|---|
| Rat[2] | 5 mg/kg | p.o. | 108 ng/mL | 1.8 h | 410 ng·h/mL | 3.8 h |
In Vivo
DBPR108 (0.01-10 mg/kg; p.o.; single dose) dose-dependently inhibits plasma DPP-4 activity (ED50 = 1.9 mg/kg) in diabetic db/db mice[2].
DBPR108 (0.01-3 mg/kg; p.o.; single dose) dose-dependently inhibits plasma DPP-4 activity (ED50 = 0.1 mg/kg) in healthy beagle dogs[2].
DBPR108 (0.1-10 mg/kg; p.o.; single dose) dose-dependently improves oral glucose tolerance (ED50 = 0.144 mg/kg) in healthy C57BL/6JNarl mice[2].
DBPR108 (0.01-10 mg/kg; p.o.; single dose) dose-dependently improves oral glucose tolerance (ED50 = 0.033 mg/kg) in DIO mice, with additive efficacy when combined with Metformin (HY-B0627)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (male, 250-300 g, glucose ingestion challenged)[2]
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Dosage:0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited plasma DPP-4 activity, with an ED50 of 0.9 mg/kg.
Significantly increased plasma active GLP-1 levels at 5 minutes post-glucose challenge, with a greater ΔAUC than vehicle control at 10 mg/kg dose.
Significantly increased plasma insulin levels at 10 minutes post-glucose challenge, with a prolonged elevation until 15 minutes and a greater ΔAUC than vehicle control at 10 mg/kg dose.
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Animal Model:BKS.Cg-m+/+Leprdb/J (db/db) (adult)[2]
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Dosage:0.01 mg/kg; 0.1 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited plasma DPP-4 activity.
Achieved an ED50 of 1.9 mg/kg for DPP-4 inhibition.
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Animal Model:Beagle (male, 9-10 months old)[2]
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Dosage:0.01 mg/kg; 0.05 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited plasma DPP-4 activity at all tested doses.
Achieved an ED50 of 0.1 mg/kg for DPP-4 inhibition.
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Animal Model:C57BL/6JNarl (both sexes, adult)[2]
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Dosage:0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently suppressed glucose-induced blood glucose elevation.
Achieved an ED50 of 0.144 mg/kg for improved glucose tolerance.
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Animal Model:C57BL/6JNarl (both sexes, fed high-fat diet for 6 months)[2]
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Dosage:0.01 mg/kg; 0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
0.1 mg/kg (in combination with 50, 100 mg/kg Metformin) -
Administration:p.o.; single dose
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Result:Dose-dependently suppressed glucose-induced blood glucose elevation.
Achieved an ED50 of 0.033 mg/kg for improved glucose tolerance.
Produced additive improvements in glucose tolerance when combined with 0.1 mg/kg DBPR108 plus 50 or 100 mg/kg metformin.
Completely suppressed glucose-induced blood glucose elevation when combined with 0.1 mg/kg DBPR108 plus 100 mg/kg metformin.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1186426-66-3
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Appearance Solid
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Peso molecular 324.39
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Fòrmula C16H25FN4O2
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Color White to off-white
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SMILES
N#C[C@H]1N(C(CNC(C)(C)CC(N2CCCC2)=O)=O)C[C@@H](F)C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : ≥ 25 mg/mL (77.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0827 mL | 15.4135 mL | 30.8271 mL | 77.0677 mL |
| 5 mM | 0.6165 mL | 3.0827 mL | 6.1654 mL | 15.4135 mL | |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0827 mL | 7.7068 mL | |
| 15 mM | 0.2055 mL | 1.0276 mL | 2.0551 mL | 5.1378 mL | |
| 20 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8534 mL | |
| 25 mM | 0.1233 mL | 0.6165 mL | 1.2331 mL | 3.0827 mL | |
| 30 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5689 mL | |
| 40 mM | 0.0771 mL | 0.3853 mL | 0.7707 mL | 1.9267 mL | |
| 50 mM | 0.0617 mL | 0.3083 mL | 0.6165 mL | 1.5414 mL | |
| 60 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL |
DBPR108 Related Classifications
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