Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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50 mg | 在庫あり | ¥ 7,500 | |||
100 mg | 在庫あり | ¥ 11,000 | |||
200 mg | 在庫あり | ¥ 13,000 | |||
500 mg | 在庫あり | ¥ 21,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 12,000 |
説明 | Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor. |
ターゲット&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]. |
別名 | Januvia, MK-0431 phosphate, Sitagliptin (phosphate) |
分子量 | 505.31 |
分子式 | C16H18F6N5O5P |
CAS No. | 654671-78-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL(49.47 mM)
You can also refer to dose conversion for different animals. 詳細
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Sitagliptin phosphate 654671-78-0 Autophagy Proteases/Proteasome DPP-4 Sitagliptin Phosphate MK-0431 MK 0431 Dipeptidyl Peptidase MK 0431 Phosphate Januvia MK0431 Inhibitor MK-0431 phosphate inhibit MK0431 Phosphate Sitagliptin DPP MK-0431 Phosphate Sitagliptin (phosphate) inhibitor