A DPP-4 inhibitor (IC50 = 18 nM); selective for DPP-4 over DPP-8 (IC50 = 48 µM) as well as several other peptidases; improves glucose tolerance in insulin-resistant Zucker fatty and high-fat diet fed rats as well as ob/ob and high-fat diet fed mice; reduces hyperglycemia in mice fed a high-fat diet with streptozotocin-induced diabetes

(–)-Sitagliptin (phosphate) – 250 mg

Brand:
Cayman
CAS:
654671-78-0
Storage:
-20
UN-No:
Non-Hazardous - /

(–)-Sitagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 18 nM).{26165} It is selective for DPP-4 over DPP-8 (IC50 = 48 µM) as well as several other peptidases, including DPP-9, DPP-2, and amino peptidase P.{26165,26164} (–)-Sitagliptin improves glucose tolerance in insulin-resistant Zucker fatty and high-fat diet fed rats as well as ob/ob and high-fat diet fed mice.{26071} It also reduces hyperglycemia in mice fed a high-fat diet with diabetes induced by streptozotocin (Item No. 13104). Formulations containing (–)-sitagliptin have been used in the treatment of type 2 diabetes mellitus.  

 

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Description

A DPP-4 inhibitor (IC50 = 18 nM); selective for DPP-4 over DPP-8 (IC50 = 48 µM) as well as several other peptidases; improves glucose tolerance in insulin-resistant Zucker fatty and high-fat diet fed rats as well as ob/ob and high-fat diet fed mice; reduces hyperglycemia in mice fed a high-fat diet with streptozotocin-induced diabetes,

Formal name: (3R)-3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-1-butanone, monophosphate

Synonyms:  (R)-Sitagliptin|INN|MK-431|ONO-5435

Molecular weight: 505.3

CAS: 654671-78-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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