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/ Linagliptin/利拉利汀

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

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

Linagliptin是一种高效、选择性的 DPP-4 抑制剂，IC50 为 1 nM，在2型糖尿病模型中具有促胰岛素激素的作用，能够激活血小板自噬并抑制铁死亡。

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

货号：A392251 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >

Linagliptin/利拉利汀 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/利拉利汀 细胞实验

Cell Line
Concentration Treated Time Description References
Human cardiomyocytes 100 mM 2 hours To evaluate the effect of Linagliptin on DPP-4-mediated titin cleavage, results showed that Linagliptin completely prevented DPP-4-induced titin cleavage. J Cell Mol Med. 2021 Jan;25(2):729-741.
Human cardiomyocytes 100 mM 30 minutes To evaluate the effect of Linagliptin on cardiomyocyte passive stiffness, results showed that Linagliptin significantly reduced cardiomyocyte passive stiffness. J Cell Mol Med. 2021 Jan;25(2):729-741.

Linagliptin/利拉利汀 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Swiss mice Morphine dependence model Intraperitoneal injection 10 and 20 mg/kg Once daily for 8 consecutive days Linagliptin significantly reduced morphine withdrawal symptoms (jumping behavior) in mice and alleviated depressive and anxiety behaviors during short-term and long-term morphine withdrawal. Molecules. 2022 Apr 12;27(8):2478
Db/db mice Type 2 diabetes model Oral 10 mg/kg Once daily for 8 weeks To assess the effect of Linagliptin on glomerular autophagy in a model of type 2 diabetes, the results showed that Linagliptin alone or in combination with Empagliflozin enhanced glomerular autophagy, mitigated glomerular sclerosis and podocyte injury, and slowed the growth of albuminuria. Int J Mol Sci. 2020 Apr 23;21(8):2987
ZSF1 rats MetS-induced cardiac disease model Oral 83 mg/kg Once daily for 4 weeks To evaluate the effect of Linagliptin on left ventricular stiffness, results showed that Linagliptin significantly improved left ventricular relaxation, reduced cardiomyocyte passive stiffness, and decreased cardiac fibrosis. J Cell Mol Med. 2021 Jan;25(2):729-741.
C57BL6/ApoE-/- mice High fat diet-induced metabolic disease model Oral gavage 10 mg/kg Once daily for 28 days To validate the regulatory effect of DPP4 inhibitor on insulin-induced vascular oxidative stress in vivo, results showed DPP4i pretreatment reversed the effects of insulin on vascular oxidative stress Sci Transl Med. 2020 Apr 29;12(541):eaav8824.

Linagliptin/利拉利汀 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/利拉利汀 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/利拉利汀 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/利拉利汀 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/利拉利汀 技术信息

CAS号668270-12-0
分子式C25H28N8O2
分子量 472.54
SMILES Code CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
MDL No. MFCD14635356
别名 利格列汀 ;BI 1356; GSK2118436
运输蓝冰
InChI Key LTXREWYXXSTFRX-QGZVFWFLSA-N
Pubchem ID 10096344
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

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/利拉利汀 纯度/质量文件 | Linagliptin/利拉利汀 生物活性 | Linagliptin/利拉利汀 动物研究 | Linagliptin/利拉利汀 临床数据 | Linagliptin/利拉利汀 参考文献 | Linagliptin/利拉利汀 实验方案 | Linagliptin/利拉利汀 技术信息

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