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利拉利汀 /Linagliptin {[allProObj[0].p_purity_real_show]}

货号：A392251 同义名： 利格列汀 / BI 1356;GSK2118436

Linagliptin, a purine and quinazoline derivative, can inhibit DPP-4 with IC50 of 1 nM. It functions as an incretin and is used as a hypoglycemic agents in the treatment of type 2 diabetes mellitus.

Linagliptin 化学结构 CAS号：668270-12-0
Linagliptin 化学结构
CAS号：668270-12-0
Linagliptin 3D分子结构
CAS号：668270-12-0
Linagliptin 化学结构 CAS号：668270-12-0
Linagliptin 3D分子结构 CAS号：668270-12-0
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Linagliptin 纯度/质量文件 产品仅供科研

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Linagliptin 生物活性

描述 Dipeptidyl peptidase 4 (DPP4) is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides, which is ubiquitously expressed on the surface of a variety of cells. DPP4 selectively cleaves N-terminal dipeptides from a variety of substrates, including cytokines, growth factors, neuropeptides, and the incretin hormones. Linagliptin is a potent and selective DPP4 inhibitor with IC50 value of 0.77 nM[12]. In vitro, Linagliptin markedly reduces LPS induced expression of IL-6 in HUVECs at concentration ranging in 1 - 10 μM[7]. Treatment with 30 nM linagliptin for 3 days significantly inhibits podocyte growth. Treatment with 100 nM Linagliptin casued an increase in cells in the G0/G1 phase at 5 days in podocytes[13]. In vivo, linagliptin significantly inhibits DPP4 activity in kidney and plasma of diabetic mice. Oral administration of linagliptin at 5 mg/kg once daily for 24 weeks restored the normal kidney structure of STZ-induced diabetic kidney fibrosis in CD-1 mice[14]. Administration of linagliptin at 83 mg/kg to female C57BL/6 mice fed a western diet for 4 months ameliorated the develop western diet induced aortic and endothelial cell stiffness[15]. Oral administration of linagliptin at 10 mg/kg for 7 weeks significantly inhibits DPP-4 activity, and increases blood GLP-1 levels in HFD-fed mice. In addition, linagliptin decreases ischemic brain damage[16].

Linagliptin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Displacement of [N-methyl-3H]scopolamine from human recombinant muscarinic M1 receptor expressed in CHO cells, IC50=0.295 μM 18052023
HEK293 cells Function assay Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition, IC50=0.37 μM 24900696
human Caco-2 cells Function assay Inhibition of DPP4 in human Caco-2 cells after 1 hr, IC50=1 nM 18485703
pig LLC-PK1 cells 100 μM Function assay Maximal inhibition of human P-glycoprotein expressed in pig LLC-PK1 cells assessed as reduction of [3H]digoxin substrate transport at 100 uM by liquid scintillation counting 23073734

Linagliptin 动物研究

Dose Rat: 1 mg/kg - 10 mg/kg[3] (p.o.) Mice: 3 mg/kg, 30 mg/kg[4] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[5]
Dose 50 mg/kg
Administration p.o.
MRT 6.29 h
AUC0→24h 35900 nmol·h/L
T1/2 18.4 h
Tmax 4 h
AUC0-inf 36400 nmol·h/L
Cmax 3680 nmol/L
AUC0-48h 36200 nmol·h/L

Linagliptin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02183376 Hepatic Insufficiency Phase 1 Completed - -
NCT01778049 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT02183532 Healthy Phase 1 Completed - -

Linagliptin 参考文献

[1]Thomas L, Eckhardt M, et al.(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.

[2]Eckhardt M, Langkopf E, et al. 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J Med Chem. 2007 Dec 27;50(26):6450-3.

[3]Sortino MA, Sinagra T, et al. Linagliptin: A thorough Characterization beyond Its Clinical Efficacy. Front Endocrinol (Lausanne). 2013 Feb 26;4:16.

[4]Kern M, Klöting N, et al. Linagliptin improves insulin sensitivity and hepatic steatosis in diet-induced obesity. PLoS One. 2012;7(6):e38744.

[5]Linagliptin

[7]Linagliptin inhibits lipopolysaccharide-stimulated interleukin-6 production, intranuclear p65 expression, and p38 mitogen-activated protein kinase phosphorylation in human umbilical vein endothelial cells

[8]Syam YM, El-Karim SSA, Nasr T, Elseginy SA, Anwar MM, Kamel MM, Ali HF. Design, Synthesis and Biological Evaluation of Spiro Cyclohexane-1,2- Quinazoline Derivatives as Potent Dipeptidyl Peptidase IV Inhibitors. Mini Rev Med Chem. 2019;19(3):250-269. doi: 10.2174/1389557517666170828121018. PMID: 28847268.

[9]Miglio G, Vitarelli G, Klein T, Benetti E. Effects of linagliptin on human immortalized podocytes: a cellular system to study dipeptidyl-peptidase 4 inhibition. Br J Pharmacol. 2017 May;174(9):809-821. doi: 10.1111/bph.13739. Epub 2017 Mar 6. PMID: 28177527; PMCID: PMC5386990.

[10]Kanasaki K, Shi S, Kanasaki M, He J, Nagai T, Nakamura Y, Ishigaki Y, Kitada M, Srivastava SP, Koya D. Linagliptin-mediated DPP-4 inhibition ameliorates kidney fibrosis in streptozotocin-induced diabetic mice by inhibiting endothelial-to-mesenchymal transition in a therapeutic regimen. Diabetes. 2014 Jun;63(6):2120-31. doi: 10.2337/db13-1029. Epub 2014 Feb 26. PMID: 24574044.

[11]Manrique C, Habibi J, Aroor AR, Sowers JR, Jia G, Hayden MR, Garro M, Martinez-Lemus LA, Ramirez-Perez FI, Klein T, Meininger GA, DeMarco VG. Dipeptidyl peptidase-4 inhibition with linagliptin prevents western diet-induced vascular abnormalities in female mice. Cardiovasc Diabetol. 2016 Jul 8;15:94. doi: 10.1186/s12933-016-0414-5. PMID: 27391040; PMCID: PMC4938903.

[12]Darsalia V, Ortsäter H, Olverling A, Darlöf E, Wolbert P, Nyström T, Klein T, Sjöholm Å, Patrone C. The DPP-4 inhibitor linagliptin counteracts stroke in the normal and diabetic mouse brain: a comparison with glimepiride. Diabetes. 2013 Apr;62(4):1289-96. doi: 10.2337/db12-0988. Epub 2012 Dec 3. PMID: 23209191; PMCID: PMC3609599.

Linagliptin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.16mL

4.23mL

2.12mL

Linagliptin 技术信息

CAS号668270-12-0
分子式C25H28N8O2
分子量 472.542
别名 利格列汀 ;BI 1356;GSK2118436;Linagliptin. trade names Tradjenta and Trajenta
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C
溶解度

DMSO: 25 mg/mL(52.91 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

0.5% hydroxyethyl cellulose+water 30 mg/mL suspension

Tags: Linagliptin | BI 1356;GSK2118436;Linagliptin. trade names Tradjenta and Trajenta | 利格列汀 | Diabete | DPP4 | AmBeed-信号通路专用抑制剂 | Linagliptin 纯度/质量文件 | Linagliptin 生物活性 | Linagliptin 细胞研究 | Linagliptin 动物研究 | Linagliptin 临床数据 | Linagliptin 参考文献 | Linagliptin 实验方案 | Linagliptin 技术信息

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