SML4487

Sitagliptin phosphate monohydrate ≥ 99% by HPLC

≥98% (HPLC)

• Synonim(y): (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine dihydrogen phosphate monohydrate, MK-0431 hydrate, MK-431
• Wzór empiryczny (zapis Hilla): C₁₆H₁₅F₆N₅O_·H3PO4·H2O
• Numer CAS: 654671-77-9
• Masa cząsteczkowa: 523.32
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: H₂O: 2 mg/mL, clear
• storage temp.: 2-8°C

Opis

Biochem/physiol Actions

Sitagliptin phosphate monohydrate (MK-0431) is a highly selective, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor (IC50 = 18 nM; >2,600-fold selectivity over DPP-8/9) that functions via reversible, competitive inhibition of the enzyme′s catalytic active site. By preventing the proteolytic inactivation of incretins (GLP-1 and GIP) with high specificity, MK-0431 achieves >90% DPP-4 inhibition within 2 hours (sustained ~80% at 24 hours), thereby enhancing glucose-dependent insulin secretion and suppressing glucagon. This pharmacodynamic profile yields a weight-neutral antidiabetic option with additive glycemic efficacy in combination with metformin or pioglitazone, while maintaining a significantly lower risk of hypoglycemia compared to sulfonylureas. Uniquely, Sitagliptin simultaneously targets hyperglycemia and systemic inflammation; it addresses metabolic syndrome-associated inflammation by suppressing intranuclear NF-κB binding and downregulating critical mediators (JNK-1, IKKβ, TLR-4, CCR-2), demonstrating distinct anti-atherogenic potential alongside metabolic control.

Disclaimer

Hygroscopic, Store with desiccant

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS08,GHS07
• Słowo ostrzegawcze: Warning
• Kody zagrożeń: H319,H373
• Ostrzeżenia: P260 - P264 - P280 - P305 + P351 + P338 - P314 - P337 + P313
• Hazard Classifications: Eye Irrit. 2 - STOT RE 2
• Narządy docelowe: Liver
• Klasa składowania: 11 - Combustible Solids
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable