Sitagliptin phosphate monohydrate ≥ 99% by HPLC

Name: Sitagliptin phosphate monohydrate ≥ 99% by HPLC
Brand: SIGMA

≥98% (HPLC)

Synonym(e):

(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

Anmelden zur Ansicht der Organisations- und Vertragspreise.

Größe auswählen

Ansicht ändern

Über diesen Artikel

Empirische Formel (Hill-System):

C₁₆H₁₅F₆N₅O_{·H₃PO₄·H₂O}

CAS-Nummer:

654671-77-9

Molekulargewicht:

523.32

UNSPSC Code:

12352200

Assay:

≥98% (HPLC)

Form:

powder

Storage condition:

desiccated

Technischer Dienst

Benötigen Sie Hilfe? Unser Team von erfahrenen Wissenschaftlern ist für Sie da.

Unterstützung erhalten

Eigenschaften

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

Beschreibung

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.