Trelagliptin(SYR472 Zafatek)

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CAS NO:	865759-25-7
规格:	≥98%

包装与价格：

包装	价格(元)
50mg	询价
100mg	询价
250mg	询价
500mg	询价
1g	询价
2g	询价

Trelagliptin (formerly also known as SYR-472; trade name Zafatek) is a potent, highly selective, long-acting DPP-4 (dipeptidyl peptidase-4) inhibitor with potential anti-hyperglycemic activity. It was under development by Takeda and approved in Japan for the treatment of type 2 diabetes (T2D). Unlike other approved drugs of the same class that are usually administered once daily, trelagliptin can be given once weekly, which is an advantage.

理化性质和储存条件

Molecular Weight (MW)	357.38
Formula	C18H20FN5O2
CAS No.	865759-25-7
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 71 mg/mL (198.7 mM)
	Water:<1 mg/mL
	Ethanol: 3 mg/mL warmed (8.4 mM)
Solubility (In vivo)	Chemical Name: (R)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile. InChi Key: IWYJYHUNXVAVAA-OAHLLOKOSA-N InChi Code: InChI=1S/C18H20FN5O2/c1-22-17(25)8-16(23-6-2-3-15(21)11-23)24(18(22)26)10-13-7-14(19)5-4-12(13)9-20/h4-5,7-8,15H,2-3,6,10-11,21H2,1H3/t15-/m1/s1 SMILES Code: N#CC1=CC=C(F)C=C1CN(C(N2C)=O)C(N3C[C@H](N)CCC3)=CC2=O
Synonyms	SYR 472; Trelagliptin; SYR-472; SYR472; trade name: Zafatek.

实验参考方法

In Vitro	In vitro activity: Trelagliptin (also known as SYR-472) is a potent, highly selective, long-acting DPP-4 (dipeptidyl peptidase-4) inhibitor under development by Takeda for the treatment of type 2 diabetes (T2D).. Once-weekly Trelagliptin treatment produced clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. It was well tolerated and might be a new treatment option for patients with this disease. Trelagliptin was approved in Japan for the treatment of type 2 diabetes mellitus (T2DM).
In Vivo	Trelagliptin improves glycaemic control by inhibition of DPP-4 activity.
Animal model
Formulation & Dosage
References	Lancet Diabetes Endocrinol. 2014 Feb;2(2):125-32.