Trelagliptin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
曲格列汀(SYR-472)是一种选择性的DPP-4抑制剂,是用于治疗2型糖尿病(T2DM)的药剂[1].
二肽基肽酶(DPP)-4,也称为腺苷脱氨酶络合蛋白2或CD26,是在大多数细胞类型的表面表达的一种抗原酶,其在调节免疫系统\信号转导和细胞凋亡方面发挥着重要作用[2, 3].
曲格列汀(SYR-472)是一种强效的DPP-4抑制剂,与其他已批准药剂类型(每日服用一次)不同,曲格列汀每周服用一次[1].已在日本开展临床试验,通过与已批准的药剂(即阿格列汀)比较来检测曲格列汀的效果.结果表明,每周服用一次曲格列汀的功效和安全性与每日服用一次的阿格列汀类似,这表明曲格列汀可能是一种有用的\每周服用一次的新抗糖尿病药物[2].
在日本,曲格列汀(SYR-472)已用于治疗2型糖尿病患者的2期和3期临床试验中,结果表明其效用和安全性与每日服用一次的阿格列汀类似,在临床上和统计学上均可显著改善血糖控制且耐受性良好[2, 3].
参考文献：
[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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 357.38 |
| Cas No. | 865759-25-7 |
| Formula | C18H20FN5O2 |
| Synonyms | SYR-472,SYR472,SYR 472,Trelagliptin |
| Solubility | ≥11.6 mg/mL in DMSO; ≥3.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥93.8 mg/mL in H2O |
| Chemical Name | 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile |
| SDF | Download SDF |
| Canonical SMILES | CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCCC(C3)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | 曲格列汀(Trelagliptin)是一种长效的二肽基肽酶-4(DPP-4)抑制剂 . | |||||
| 靶点 | DPP-4 | |||||
| IC50 | ||||||
质量控制和MSDS
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化学结构
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