Teneligliptin

Teneligliptin is a potent DPP-4 inhibitor API used in the treatment of type 2 diabetes mellitus. As a competitive inhibitor of DPP-4, Teneligliptin prolongs the half-life of endogenous incretin hormones—glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)—thereby enhancing glucose-dependent insulin secretion and suppressing glucagon release. The clinical profile of Teneligliptin is characterized by its long duration of action (half-life of approximately 18 hours) and potent in vitro activity, with IC₅₀ values of approximately 1 nM against human plasma and rat plasma DPP-4. In quality control contexts, Teneligliptin is subject to stringent impurity profiling to ensure the purity, safety, and efficacy of teneligliptin-containing drug products. As a key API for diabetes management, Teneligliptin continues to expand its global footprint with growing clinical evidence supporting its efficacy and safety profile in diverse patient populations.

 

Product Parameters

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Parameter	Specification
Product Name	Teneligliptin
CAS Number	760937-92-6
Molecular Formula	C₂₂H₃₀N₆OS
Molecular Weight	426.58 g/mol
Physical Form	Crystalline solid
Melting Point	>100 °C (dec.)
Boiling Point	663.4 ± 55.0 °C (Predicted)
Density	1.38 g/cm³
Solubility	Slightly soluble in water; Soluble in ethanol and diethyl ether; Soluble in DMSO
Storage Condition	Refrigerator (2–8 °C)

 

Synthetic Route

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Teneligliptin is synthesized from N-Boc piperazine and diacetylone via condensation, cyclization, and deprotection to yield the intermediate 1-(3-methyl-1-phenyl-1H-pyrazolo-5-yl)piperazine; followed by Fmoc protection, oxidation, and condensation of trans-4-hydroxy-L-proline to obtain intermediate 3-[[(2S)-1-(9H-fluoromethoxy-9-yl)carbonyl]-4-oxopyrrolidin-2-carbonyl]thiazolidine. These two intermediates are subsequently reduced via amination and deprotection to produce the antidiabetic drug trelitin, with a total yield of 47.2% (based on trans-4-hydroxy-L-proline) and purity of 99.1% (as determined by HPLC). The structure of trelitin was confirmed by MS, IR, 1H-NMR, and 13C-NMR spectra. This synthetic route employs inexpensive and readily available starting materials, mild reaction conditions, simple post-processing steps, and high yields, laying a solid foundation for pilot-scale production.

 

Why Cosperpharm?

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When your diabetes therapeutic manufacturing program demands a DPP-4 inhibitor API with verified stereochemical purity and comprehensive documentation, Cosperpharm delivers Teneligliptin with the analytical rigor and supply chain reliability that pharmaceutical customers require.

 

Quality begins with the stereochemistry. The (2S,4S) configuration in Teneligliptin is critical for DPP-4 binding affinity—any epimerization at either stereocenter significantly reduces potency and introduces difficult-to-remove impurities. Our analytical release protocol includes chiral HPLC for stereoisomer control, HPLC purity verification, residual solvent analysis, and water content determination.

 

Documentation that supports regulatory submission. As a DPP-4 inhibitor API, Teneligliptin requires comprehensive documentation for regulatory filings. Every shipment includes a Certificate of Analysis (COA) with batch-specific purity data, chromatographic traceability, and residual solvent analysis. DMF-ready documentation, stability summaries, and custom quality agreements are available upon request.

 

Flexible supply across all development stages. Cosperpharm supplies Teneligliptin from gram-scale R&D quantities for process development and analytical method validation to multi-kilogram batches for commercial API manufacturing. R&D samples ship within 5–7 business days; bulk orders ship within 2–3 weeks.

 

Technical support for the full synthetic cascade. Our process chemistry team can advise on the stereoselective synthesis of the thiazolidine-piperazine scaffold, purification strategies for removing process-related impurities, and analytical methods for enantiomeric purity determination.

 

Global reach with transparent pricing. Cosperpharm ships to pharmaceutical manufacturers, CROs, and analytical laboratories worldwide, with full customs documentation included. Volume discounts apply at commercial scales.

 

Storage Conditions

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Store Teneligliptin in a tightly sealed container under refrigeration (2–8 °C). Keep the container dry, protected from light, and stored in a clean, well-ventilated area away from strong oxidizing agents and sources of ignition.

 

Shelf life: Stability data available upon request to support regulatory filings.

 

Handling precautions: Use only in a fume hood. Wear chemical-resistant gloves, safety goggles, and a lab coat. Avoid generating dust or aerosols. Do not eat, drink or smoke in work areas. After handling, wash hands thoroughly. Refer to the Safety Data Sheet (SDS) for complete safety information.

 

Contact Us

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Interested in Teneligliptin for your diabetes therapeutic manufacturing or analytical development program? Contact Cosperpharm today. Our team is ready to provide product specifications, documentation, and pricing tailored to your requirements.