| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Retagliptin targets dipeptidyl peptidase 4 (DPP-4), an enzyme responsible for degrading incretin hormones such as GLP-1 and GIP. DPP-4 is a serine protease that cleaves and inactivates incretins. Retagliptin is a selective, competitive inhibitor of DPP-4. By inhibiting DPP-4, Retagliptin prolongs the half-life of incretins, enhancing insulin secretion and reducing glucagon release in a glucose-dependent manner. This improves glycemic control in patients with type 2 diabetes.
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| ln Vitro |
One class of chemicals used in type 2 diabetes research is resagliptin. Repagliptin increases the effects of incretin by preventing GLP-1 from being broken down [1].
In vitro, Retagliptin has been shown to selectively and competitively inhibit DPP-4 activity. Its activity is typically measured using enzyme assays with recombinant DPP-4 and a fluorogenic or chromogenic substrate. The compound's ability to inhibit DPP-4-mediated substrate cleavage is measured, and the IC50 is determined. These in vitro studies confirm Retagliptin's potent and selective DPP-4 inhibitory activity. |
| ln Vivo |
In vivo, Retagliptin has been investigated as a therapeutic candidate for type 2 diabetes mellitus. By inhibiting DPP-4, it prolongs incretin signaling, enhancing insulin secretion and reducing glucagon release. Retagliptin has been developed to improve glycemic control with minimal risk of hypoglycemia. It is a relatively new drug that has gained popularity due to its efficacy and safety profile. Retagliptin is used in the research and study of type 2 diabetes.
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| Enzyme Assay |
In vitro enzyme assays for Retagliptin measure its inhibition of DPP-4 activity. DPP-4 enzyme is incubated with a fluorogenic or chromogenic substrate (e.g., Gly-Pro-pNA) in the presence of varying concentrations of Retagliptin. The cleavage of the substrate produces a signal that is measured, and the IC50 is determined from the dose-response curve. Selectivity can be assessed by testing the compound against other proteases. These assays confirm Retagliptin's potent DPP-4 inhibitory activity.
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| Cell Assay |
In vitro cell-based assays for Retagliptin are used to study its effects on incretin degradation and insulin secretion. Cells expressing DPP-4 (e.g., intestinal epithelial cells) or pancreatic β-cells are treated with Retagliptin, and the degradation of GLP-1 or GIP is measured. Insulin secretion from β-cells can be measured using ELISA. These assays confirm the compound's cellular activity as a DPP-4 inhibitor and its effects on incretin-mediated insulin secretion.
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| Animal Protocol |
In vivo animal experiments for Retagliptin are conducted in animal models of type 2 diabetes, such as diet-induced obese mice or genetically diabetic mice. In a typical study, Retagliptin is administered orally, and blood glucose levels are measured. Glucose tolerance tests and insulin tolerance tests are performed to assess the compound's effects on glucose metabolism. These studies confirm the in vivo efficacy of Retagliptin as a DPP-4 inhibitor.
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| ADME/Pharmacokinetics |
Retagliptin has a molecular weight of 464.36 g/mol. It is a solid compound. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic properties have been characterized. Retagliptin is orally bioactive. Detailed pharmacokinetic parameters, such as half-life and bioavailability, are available from clinical studies.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Retagliptin is not provided in standard product descriptions. As a DPP-4 inhibitor, its safety profile is expected to be similar to other drugs in this class, which are generally well-tolerated. Common side effects may include gastrointestinal disturbances and headache. However, specific toxicity data, such as adverse effects or organ toxicity, are not detailed. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
Retagliptin is being investigated in the clinical trial NCT02822534 (SP2086 Pharmacokinetic and Pharmacodynamic Study of Single and Multiple Doses in Patients with Type 2 Diabetes).
Retagliptin (SP2086) is a selective, competitive, and orally bioactive DPP-4 inhibitor. It is a DPP-4 inhibitor potentially used to treat Type 2 diabetes mellitus. By blocking DPP-4 activity, it prolongs incretin signaling, enhancing insulin secretion and reducing glucagon release. It aims to improve glycemic control with minimal risk of hypoglycemia. Retagliptin is a relatively new drug that has gained popularity due to its efficacy and safety profile. It is used in the research of type 2 diabetes. |
| Exact Mass |
464.128
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|---|---|
| CAS # |
1174122-54-3
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| Related CAS # |
Retagliptin phosphate;1256756-88-3
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| PubChem CID |
44193830
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
587.8±50.0 °C at 760 mmHg
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| Flash Point |
309.3±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.570
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| LogP |
1.84
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
699
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC(C1=NC(C(=O)OC)=C2CN(C(C[C@@H](CC3C=C(C(=CC=3F)F)F)N)=O)CCN21)(F)F
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| InChi Key |
WIIAMRXFUJLYEF-SNVBAGLBSA-N
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| InChi Code |
InChI=1S/C19H18F6N4O3/c1-32-17(31)16-14-8-28(2-3-29(14)18(27-16)19(23,24)25)15(30)6-10(26)4-9-5-12(21)13(22)7-11(9)20/h5,7,10H,2-4,6,8,26H2,1H3/t10-/m1/s1
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| Chemical Name |
methyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-6,8-dihydro-5H-imidazo[1,5-a]pyrazine-1-carboxylate
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| Synonyms |
SP-2086 SP 2086Retagliptin SP2086
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~215.35 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04667143 | UNKNOWN STATUS | Drug: Retagliptin, Henagliflozein, metformin XR | Diabetes Mellitus, Type II | Jiangsu HengRui Medicine Co., Ltd. | 2021-01 | Phase 3 |
| NCT05054842 | ACTIVE, NOT RECRUITING | Drug: Retagliptin phosphate tablets、metformin sustained-release tablets Drug: Retagliptin phosphate placebo tablets、 metformin sustained-release tablets |
Type 2 Diabetes | Jiangsu HengRui Medicine Co., Ltd. | 2021-12-06 | Phase 3 |
| NCT02500485 | UNKNOWN STATUS | Drug: SHR3824, SP2086 | Type 2 Diabetes | Jiangsu HengRui Medicine Co., Ltd. | 2015-05 | Phase 1 |
| NCT05415644 | COMPLETED | Drug: hrx0701 tablets、Metformin hydrochloride tablets、Retagliptin phosphate tablets Drug: hrx0701 tablets |
Type 2 Diabetes Mellitus | Shandong Suncadia Medicine Co., Ltd. | 2022-07-05 | Phase 1 |
| NCT06035406 | NOT YET RECRUITING | Drug: Retagliptin Phosphate Tablet | Diabetes | Jiangsu HengRui Medicine Co., Ltd. | 2023-09 | Phase 1 |
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