Trelagliptin|865759-25-7|(曲格列汀; SYR-472)-陌孚医药/Medlife

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Trelagliptin (Synonyms: 曲格列汀; SYR-472)

目录号: PL13893 纯度: ≥99%

CAS No. :865759-25-7

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中文名称	Trelagliptin
中文别名	曲格列汀;曲格列汀 TRELAGLIPTIN;2-[[6-[(3R)-3-氨基-1-哌啶基]-3,4-二氢-3-甲基-2,4-二氧代-1(2H)-嘧啶基]甲基]-4-氟-苯甲腈;游离的曲格列汀;曲格列汀杂质G;曲格列汀-INT E;曲格列汀1;(R)-2-((6-(1-(3-胺哌啶基)-3-甲基-2,4-二氧杂-3,4-二氢吡啶基-1-(2H)-基)甲基)-4-氟苯甲氰;S)-2-((6-(3-氨基哌啶-1-基)-3-甲基-2,4-二氧杂-3,4-二氢嘧啶-1(2H)-基)甲基)-4-氟苯甲氰;Trelagliptin 抑制剂;曲格列汀游离碱;曲格列汀杂质;他达那非
英文名称	Trelagliptin
英文别名	Trelagliptin;Trelagliptin(syr472);Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H) -pyrimidinyl]methyl]-4-fluoro-;Trelagliptin (R)-2-[[6-(3-Aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl]-4-fluorobenzonitrile;(S)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile;Trelagliptin Isomer Impurity;Trelagliptin free base;2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile;Trelagliplin;SYR 472;SYR-472;Trelagliptin (USAN);UNII-Q836OWG55H;Trelagliptin IMpurity
Cas No.	865759-25-7
分子式	C₁₈H₂₀FN₅O₂
分子量	357.38
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Trelagliptin (SYR-472) 是一种有效的，具有口服活性 DPP-4 抑制剂，IC₅₀ 为 4 nM。Trelagliptin (SYR-472) 改善体内血糖控制，可用于2 型糖尿病 (T2DM) 的研究。

生物活性

Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC 50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).

性状

Solid

IC50 & Target[1][2]

IC50: 4 nM (DPP-4)

体外研究(In Vitro)

Dipeptidyl peptidase-4 (DPP-4) is one of the widely explored novel targets for type 2 diabetes mellitus (T2DM) strategy to preserve the endogenous glucagon like peptide (GLP)-1 activity by inhibiting the DPP-4 action.
Trelagliptin exhibits potent inhibitory activity toward DPP-4 prepared from Caco-2 cells with an IC50 value of 5.4 nM. Trelagliptin also inhibits human, dog, and rat plasma DPP-4 activity with IC50 values of 4.2 nM, 6.2 nM, and 9.7 nM, respectively.
Trelagliptin is highly selective for DPP-4 and displays IC50 values >100,000 nM corresponding to >10,000-fold selectivity over DPP-2, DPP-8, DPP-9, PEP and FAPα activities. Trelagliptin shows DPP4 selective about 4- and 12-fold more potent than alogliptin (HY-A0023) and sitagliptin (HY-13749), respectively.

体内研究(In Vivo)

Trelagliptin (oral gavage; 7 mg/kg; single dose) shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h.
Trelagliptin (oral gavage; 3 mg/kg; single dose; 60 min prior to oral glucose) significantly improves the glucose tolerance capacity by decreasing the AUC 0?120min of 19.3% compared with the vehicle group in ob/ob mice.
Trelagliptin (oral gavage; 10 mg/kg; once a week; 8 weeks) caused significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 16.8% compared to the control.It also increases insulin level and raised it by 1.7-fold in AUC 0?120min in ob/ob mice.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Bhumika D Patel, et al. Recent approaches to medicinal chemistry and therapeutic potential of dipeptidyl peptidase-4 (DPP-4) inhibitors. Eur J Med Chem. 2014 Mar 3;74:574-605.
[2]. Charles E Grimshaw, et al. Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism. PLoS One. 2016 Jun 21;11(6):e0157509.

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (139.91 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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