| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Teneligliptin hydrobromide hydrate targets the enzyme dipeptidyl peptidase-4 (DPP-4). DPP-4 is a serine protease responsible for the rapid degradation of incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, teneligliptin increases the half-life and bioavailability of these incretins, thereby enhancing glucose-dependent insulin secretion and suppressing glucagon release, which leads to improved glycemic control.
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| ln Vitro |
In vitro, Teneligliptin hydrobromide hydrate competitively inhibits human plasma, rat plasma, and human recombinant DPP-4. It is a potent inhibitor, with IC50 values of approximately 1 nM. More specifically, it has been reported to have IC50 values of 0.37 nM and 0.29 nM for the human and rat enzymes, respectively. This high potency makes it an effective compound for blocking DPP-4 activity in vitro.
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| ln Vivo |
In vivo, Teneligliptin has demonstrated efficacy in improving postprandial hyperglycemia and dyslipidemia after single and repeated administrations in preclinical models. As an orally bioavailable drug, it is effective in lowering blood glucose levels in animal models of type 2 diabetes. Its long-lasting action allows for once-daily dosing in clinical settings. The compound has been approved for the treatment of type 2 diabetes mellitus in Japan.
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| Enzyme Assay |
The in vitro activity of Teneligliptin hydrobromide hydrate is typically measured in a DPP-4 enzyme inhibition assay. In this assay, a recombinant DPP-4 enzyme or plasma containing the enzyme is incubated with a fluorogenic substrate and varying concentrations of the test compound. The enzyme cleaves the substrate to release a fluorescent product. The inhibition of this activity by the compound is measured, and the IC50, the concentration required to inhibit 50% of the enzyme activity, is calculated from the dose-response curve.
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| Cell Assay |
Cellular assays for DPP-4 inhibitors are often performed using cell lines that express DPP-4 on their surface, such as Caco-2 cells. Cells are treated with the inhibitor, and the DPP-4 activity on the cell surface or in the culture supernatant is measured. The compound's ability to inhibit cellular DPP-4 activity is then quantified. In addition, the effect of the inhibitor on incretin degradation can be assessed in cell-based systems.
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| Animal Protocol |
In vivo efficacy of Teneligliptin hydrobromide hydrate is evaluated in animal models of type 2 diabetes, such as the Zucker diabetic fatty (ZDF) rat or db/db mouse. The compound is administered orally, and its effects on blood glucose levels, oral glucose tolerance, and plasma insulin and incretin levels are measured. The long-lasting nature of the compound is also assessed by measuring its pharmacodynamic effects over a 24-hour period after a single dose.
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| ADME/Pharmacokinetics |
Teneligliptin hydrobromide hydrate is an orally bioavailable small molecule. It is well-absorbed after oral administration and has a long duration of action, allowing for once-daily dosing. The compound is metabolized in the liver, primarily by CYP450 enzymes, and is excreted in the urine and feces. Its pharmacokinetic properties, such as half-life, clearance, and volume of distribution, have been well-characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Teneligliptin is generally well-tolerated in clinical use. Common adverse effects may include nasopharyngitis, headache, and gastrointestinal disturbances. As with other DPP-4 inhibitors, it has a low risk of hypoglycemia. Its safety profile has been established through extensive clinical trials and post-marketing surveillance. The compound is contraindicated in patients with a history of severe hypersensitivity to the drug.
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| References |
Diabetes Metab Syndr Obes.2013 May 6;6:187-95;J Endocrinol.2015 Oct;227(1):25-36. |
| Additional Infomation |
Teneligliptin hydrobromide hydrate is a potent, competitive, and long-lasting DPP-4 inhibitor. It is a valuable therapeutic option for the treatment of type 2 diabetes mellitus, particularly in Japan where it is approved under the trade name Tenelia. Its unique chemotype and long duration of action distinguish it from other DPP-4 inhibitors.
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| Molecular Formula |
C44H67BR5N12O3S2
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|---|---|
| Molecular Weight |
1275.73138260841
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| Exact Mass |
1270.081
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| CAS # |
1572583-29-9
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| Related CAS # |
Teneligliptin;760937-92-6;Teneligliptin hydrobromide;906093-29-6
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| PubChem CID |
53297474
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
66
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| Complexity |
594
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=NN(C(=C1)N2CCN(CC2)[C@H]3C[C@H](NC3)C(=O)N4CCSC4)C5=CC=CC=C5.CC1=NN(C(=C1)N2CCN(CC2)[C@H]3C[C@H](NC3)C(=O)N4CCSC4)C5=CC=CC=C5.O.Br.Br.Br.Br.Br
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| InChi Key |
NQPRXLXVOBOTGT-KSLCDFCZSA-N
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| InChi Code |
InChI=1S/2C22H30N6OS.5BrH.H2O/c2*1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27;;;;;;/h2*2-6,13,19-20,23H,7-12,14-16H2,1H3;5*1H;1H2/t2*19-,20-;;;;;;/m00....../s1
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| Chemical Name |
[(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone;hydrate;pentahydrobromide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
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 | 0.7839 mL | 3.9193 mL | 7.8386 mL | |
| 5 mM | 0.1568 mL | 0.7839 mL | 1.5677 mL | |
| 10 mM | 0.0784 mL | 0.3919 mL | 0.7839 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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