| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Dipeptidyl peptidase-4 (DPP-4). Fotagliptin selectively inhibits DPP-4, the enzyme responsible for degrading incretin hormones GLP-1 and GIP. By inhibiting DPP-4, fotagliptin increases plasma GLP-1 levels, enhancing glucose-dependent insulin secretion and suppressing glucagon release, thereby improving glycemic control.
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|---|---|
| ln Vitro |
Fotagliptin is a potent DPP-4 inhibitor with an IC50 of 2.27 nM. In vitro, it inhibits DPP-4 activity in human plasma or recombinant enzyme assays, leading to increased GLP-1 levels. It is selective for DPP-4 over other related proteases.
|
| ln Vivo |
In vivo, fotagliptin is orally active and demonstrates safety in rats and dogs. It achieves high DPP-4 inhibition and increases plasma GLP-1 levels. Clinical trials have shown efficacy in reducing HbA1c and fasting plasma glucose in patients with T2D when used as add-on therapy to metformin.
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| Enzyme Assay |
DPP-4 inhibition assays use recombinant human DPP-4 or human plasma incubated with a fluorogenic substrate (e.g., Gly-Pro-AMC). Fotagliptin is added at varying concentrations, and the rate of AMC release is measured fluorometrically. IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cell assays for fotagliptin include measuring GLP-1 secretion from enteroendocrine L-cells (e.g., GLUTag cells) after DPP-4 inhibition. Insulin secretion from pancreatic β-cells can be assessed in response to glucose and GLP-1.
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| Animal Protocol |
In vivo animal protocols for fotagliptin use rat or dog models. The compound is administered orally by gavage. Plasma DPP-4 activity is measured using a fluorogenic substrate. Plasma GLP-1 and insulin levels are quantified by ELISA. Glucose tolerance tests are performed.
|
| Exact Mass |
342.16
|
|---|---|
| CAS # |
312954-58-7
|
| Related CAS # |
1403496-40-1 (benzoate);312954-58-7;
|
| PubChem CID |
53258570
|
| Appearance |
Typically exists as solid at room temperature
|
| tPSA |
98.1
|
| Hydrogen Bond Donor Count |
1
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
638
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC1=NN=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCC[C@H](C3)N
|
| InChi Key |
IXSWMXRAIPXMRH-OAHLLOKOSA-N
|
| InChi Code |
InChI=1S/C17H19FN6O/c1-11-16(25)24(9-13-7-14(18)5-4-12(13)8-19)17(22-21-11)23-6-2-3-15(20)10-23/h4-5,7,15H,2-3,6,9-10,20H2,1H3/t15-/m1/s1
|
| Chemical Name |
2-[[3-[(3R)-3-aminopiperidin-1-yl]-6-methyl-5-oxo-1,2,4-triazin-4-yl]methyl]-4-fluorobenzonitrile
|
| 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.) |
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.
Link: https://clinicaltrials.gov/ct2/show/NCT06883656
Conditions:Type 2 Diabetes Mellitus (T2DM)|Renal InsuficiencyLink: https://clinicaltrials.gov/ct2/show/NCT05801627
Conditions:Diabetes Mellitus, Type 2Link: https://clinicaltrials.gov/ct2/show/NCT05782192
Conditions:Diabetes Mellitus, Type 2Products are for research use only; We do not sell to patients
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