CAS Number:486460‑32‑6
Synonyms: Sitagliptin free base; (R)-7‑[(3‑Trifluoromethyl‑5,6‑dihydro[1,2,4]triazolo[4,3‑a]pyrazin‑7‑yl)amino]‑3‑(2,4,5‑trifluorophenyl)‑4‑oxo‑1‑butanamine
Chemical Formula:C₁₆H₁₅F₆N₅O
Molecular Weight:419.3 g/mol
Product Introduction
A white to off-white, non‑hygroscopic powder that serves as the API precursor for sitagliptin phosphate tablets (e.g., Januvia). Sitagliptin is an oral DPP‑4 inhibitor used to improve glycemic control in adults with type 2 diabetes
| Property | Value |
|---|---|
| Appearance | White to off‑white powder |
| Solubility | Soluble in methanol; slight solubility in water |
| Melting Point | N/A (typically characterized via powder diffraction) |
| pKₐ (amine) | Basic; typical secondary amine range (~9–10) |
| Bioavailability (phosphate salt) | ~87% when dosed orally |
| Protein Binding | ~38% |
| Half‑life (phosphate salt) | 8–14 h |
| Excretion | ~79% unchanged via kidneys |