Sitagliptin

Synonyme: (3R)-3-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one, Januvia, Xelevia, Tesavel, Sitagliptin phosphate

Sitagliptin is a highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor that enhances incretin hormone activity. Its structure features a trifluorophenyl β-amino ketone linked to a triazolopyrazine ring, a combination that yields nanomolar potency and excellent target selectivity. The compound is typically manufactured as the phosphate salt (CAS 654671-78-0) to improve aqueous solubility and oral bioavailability.

First approved in 2006, sitagliptin remains a cornerstone in type 2 diabetes management. It is available in various polymorphic forms, with Form I being the most thermodynamically stable and widely used in solid dosage forms. The API is produced under cGMP conditions and is characterized by high chiral purity, with the (R)-enantiomer as the active configuration.

As a leading DPP-4 inhibitor, sitagliptin serves as a reference standard in analytical labs and a key active ingredient in fixed-dose combinations with metformin. Its well-established safety profile and predictable pharmacokinetics make it a preferred choice for formulators targeting glycemic control.

Chemical Structure & Properties

Sitagliptin’s molecular framework consists of a trifluoromethyl-substituted triazolopyrazine fused ring attached to a β-amino ketone side chain bearing a 2,4,5-trifluorophenyl group. This arrangement creates a rigid, lipophilic scaffold that fits snugly into the DPP-4 active site. The free base has a molecular weight of 407.31 g/mol and is practically insoluble in water, but the phosphate salt markedly improves solubility, facilitating oral administration.

Mechanism of Action

• DPP-4 inhibition: Reversibly binds to the catalytic site of DPP-4, blocking the degradation of GLP-1 and GIP.
• Incretin enhancement: Increases active GLP-1 levels, leading to glucose-dependent insulin secretion.
• Glucagon suppression: Reduces glucagon release from pancreatic alpha cells, lowering hepatic glucose output.
• Gastric emptying: Slows nutrient absorption, contributing to postprandial glucose control.

Quality Specifications (QC Tests)

Supply & Documentation

• Capacity: 5 metric tons per year
• Lieferzeit: 3–5 Werktage (Lagerware)
• Dokumentation: COA, MSDS, TDS available upon request
• Verpackung: 25 kg fiber drum with double polyethylene liner

Häufig gestellte Fragen

What is the minimum order quantity?

Our MOQ is 1 kg for pilot trials and 25 kg for commercial orders.

What is the lead time for bulk orders?

Standard lead time is 3-5 business days after order confirmation.

Do you provide samples and COA?

Yes, we offer free samples (up to 50 g) with a full COA for evaluation.

Contact & Ordering Information

• Company: LyvBio Co., Ltd.
• Address: Room 5-0203, Courtyard 205, Lianhu District, Xi’an, Shaanxi, China
• Email: info@lyvbio.com
• Phone: +86-29-65816888

Learn more about our quality control and certifications, oder send us your specification for a quotation.