Cofrogliptin
Based on 1 Customer Validation
Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .
For research use only. We do not sell to patients.
- Purity: 99.29%
- CAS No.: 1844874-26-5
- Formula: C18H19F5N4O3S
- Molecular Weight:466.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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DPP-4 |
Cofrogliptin (compound 2) (Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg) increases of half-lives, has high oral exposure, low i.v. clearance and hepatic microsomal clearance after intravenous dosing.
Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) exhibits longe inhibition time of DPP-4 and decreases HbA1c level at the doses of 3 and 10 mg/kg in ob/ob mice. Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) also has a great potential of biweekly regimen for T2DM as indicated in rhesus monkeys[2].
Pharmacokinetic Parameters in ICR mice[2]
| IV(dose: 0.5 mg/kg) | PO(dose: 2 mg/kg) | |||||||
| CI(mL/min/kg) | Vdss(L/kg) | t1/2(h) | Cmax(ng/mL) | t1/2(h) | AUC0-t(ng h/mL) | F% | ||
| Omarigliptin | 7.39±2.1 | 1.65±0.27 | 3.05±0.6 | 798±122 | 4.65±1.4 | 4095±552 | 95.0±29 | |
| Cofrogliptin (compound 2) | 2.57±0.09 | 3.30±0.33 | 25.6±9.6 | 352±20 | 29.9±3.2 | 7898±873 | 62.2±6.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ob/ob mice[2]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Result:Exhibited strong inhibition capability of plasma DPP-4 in a dose dependent manner.
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Animal Model:rhesus monkeys[2]
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Dosage:10 mg/kg
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Administration:Single, orally, 10 mg/kg
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Result:Possessed the capability of plasma DPP-4 inhibition over 80% for at least 12 days.
Remained the plasma DPP-4 inhibition rates of 76.16% and 43.41%, respectively at the end of second week and third week after administration.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1844874-26-5
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Appearance Solid
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Molecular Weight 466.43
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Formula C18H19F5N4O3S
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Color White to off-white
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SMILES
FC(F)([C@@H](O[C@]1([H])C(C=C2F)=C(C=C2)F)[C@@](N(CC3=N4)CC3=CN4[S](C)(=O)=O)([H])C[C@@H]1N)F
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Synonyms
HSK7653
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (214.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 1.25 mg/mL (2.68 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.68 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1439 mL | 10.7197 mL | 21.4394 mL | 53.5986 mL |
| 5 mM | 0.4288 mL | 2.1439 mL | 4.2879 mL | 10.7197 mL | |
| 10 mM | 0.2144 mL | 1.0720 mL | 2.1439 mL | 5.3599 mL | |
| 15 mM | 0.1429 mL | 0.7146 mL | 1.4293 mL | 3.5732 mL | |
| 20 mM | 0.1072 mL | 0.5360 mL | 1.0720 mL | 2.6799 mL | |
| 25 mM | 0.0858 mL | 0.4288 mL | 0.8576 mL | 2.1439 mL | |
| 30 mM | 0.0715 mL | 0.3573 mL | 0.7146 mL | 1.7866 mL | |
| 40 mM | 0.0536 mL | 0.2680 mL | 0.5360 mL | 1.3400 mL | |
| 50 mM | 0.0429 mL | 0.2144 mL | 0.4288 mL | 1.0720 mL | |
| 60 mM | 0.0357 mL | 0.1787 mL | 0.3573 mL | 0.8933 mL | |
| 80 mM | 0.0268 mL | 0.1340 mL | 0.2680 mL | 0.6700 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.5360 mL |
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