Trelagliptin

目录号: GC16613纯度: >99.50%同义词: 曲格列汀; SYR-472
A DDP-4 inhibitor

Trelagliptin
Cas No.: 865759-25-7
规格价格库存数量操作
1mg¥172.00现货
1
5mg¥350.00现货
1
10mg¥490.00现货
1
50mg¥840.00现货
1
100mg¥1,120.00现货
1
500mg¥2,779.00现货
1
10mM (in 1mL DMSO)¥275.00现货
1

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产品描述 Description

Trelagliptin (SYR-472) is a selective inhibitor of DPP-4 and is developed for the treatment of type 2 diabetes mellitus (T2DM) [1].

Dipeptidyl peptidase (DPP)-4 also known as adenosine deaminase complexing protein 2 or CD26 is an antigenic enzyme that expressed on the surface of most cell types and plays an important role in regulating immune system, signal transduction and apoptosis [2, 3].

Trelagliptin (SYR-472) is a potent DPP-4 inhibitor and can be administered once weekly which unlike its other class approved agents that be taken once daily [1]. In Japan, clinical trials had been conducted to detect the effectiveness of Trelagliptin by comparing with the approved medicine—alogliptin and it was shown that Trelagliptin once-weekly exhibited similar efficacy and safety to alogliptin once daily, which indicated that Trelagliptin could be a useful new antidiabetes drug that needs to be given once a week [2].

Trelagliptin (SYR-472) has been used in phase 2 and phase 3 clinical trials for the treatment of patients with T2DM showed similar efficacy and safety to alogliptin once daily and produced clinically and statistically significant improvements in glycaemic control with well tolerated in Japan [2, 3].

References:
[1].  McKeage, K., Trelagliptin: First Global Approval. Drugs, 2015. 75(10): p. 1161-4.
[2].  Inagaki, N., et al., Once-weekly trelagliptin versus daily alogliptin in Japanese patients with type 2 diabetes: a randomised, double-blind, phase 3, non-inferiority study. Lancet Diabetes Endocrinol, 2015. 3(3): p. 191-7.
[3].  Inagaki, N., et al., SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet Diabetes Endocrinol, 2014. 2(2): p. 125-32.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
865759-25-7
同义词
曲格列汀; SYR-472
化学名
2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile
SMILES
CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCCC(C3)N
分子式
C18H20FN5O2
分子量
357.38 g/mol
溶解性
≥ 11.6 mg/mL in DMSO, ≥ 3.68 mg/mL in EtOH with ultrasonic and warming, ≥ 93.8 mg/mL in Water
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol