Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sitagliptin phosphate [654671-78-0]
Referência T23358-500mg
Tamanho : 500mg
Marca : TargetMol
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Sitagliptin phosphate
Catalog No. T23358 CAS 654671-78-0
Synonyms: Januvia, MK-0431 phosphate, Sitagliptin (phosphate)
Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.
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Sitagliptin phosphate, CAS 654671-78-0
| Description | Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor. |
| Targets&IC50 | DPP4:19 nM |
| In vitro | In vitro: Sitagliptin was a potent inhibitor for DPP-4 with an IC50 of 18 nM. Sitagliptin inhibited DPP-8 (IC50: 48 μM). Sitagliptin showed no effect on several related peptidases, including DPP-9, DPP-II, and aminopeptidase P [1]. |
| In vivo | In free-fed Han-Wistar rats, the ED50 values ??for the inhibition of plasma DPP-4 activity by sitagliptin phosphate were calculated as 7 hours post-dose at 2.3 mg/kg and 24 hours post-dose at 30 mg/kg [1]. A mouse model of streptozotocin-induced type 1 diabetes showed elevated plasma DPP-4 levels, which was significantly suppressed in mice on a sitagliptin phosphate diet. This is achieved through a positive effect on hyperglycemia regulation, possibly by prolonging islet graft survival. The plasma clearance and volume of distribution of sitagliptin phosphate in rats (40-48 mL/min/kg, 7-9 L/kg) were higher than those in dogs (9 mL/min/kg, 3 L/kg); its The half-life is shorter in rats, 2 hours in dogs and 4 hours in dogs[2]. |
| Synonyms | Januvia, MK-0431 phosphate, Sitagliptin (phosphate) |
| Molecular Weight | 505.31 |
| Formula | C16H18F6N5O5P |
| CAS No. | 654671-78-0 |
Storage
Solubility Information
DMSO: 25 mg/mL(49.47 mM)
References and Literature
1. Thomas L, Eckhardt M, Langkopf E, Tadayyon M, Himmelsbach F, Mark M. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. 2. Kim SJ, Nian C, Doudet DJ, McIntosh CH. Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes. 2009 Mar;58(3):641-51.