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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Linagliptin
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
668270-12-0
- 规格：
5mg
| 基本信息 | |
| CAS | No.668270-12-0 |
| 中文名称 | 利拉利汀 |
| 英文名称 | Linagliptin |
| 别名 | BI 1356 |
| 分子式 | C25H28N8O2 |
| 分子量 | 472.54 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 1308068-626-2 |
| MDL | MFCD14635356 |
| SMILES | CC#CCN1C2=C(N=C1N3CCCC(C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C |
| InChIKey | LTXREWYXXSTFRX-QGZVFWFLSA-N |
| InChI | InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7，10-11，17H，8-9，12-15，26H2，1-3H3/t17-/m1/s1 |
| PubChem CID | 10096344 |
| 靶点 | Dipeptidyl Peptidase(DPP-4) |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | Linagliptin 是一种有效，选择性的 DPP-4 抑制剂。 |
| 生物活性 | Linagliptin is a highly potent， selective DPP-4 inhibitor with IC50 of 1 nM.[1-4] |
| IC50 | IC50: 1 nM (DPP-4)[1-4] |
| In Vitro | Linagliptin inhibits DPP-4 activity in vitro in several independent experiments with IC50 values of 0.4， 0.5， 0.9， and 1.1 nM (mean IC50， approximately 1 nM). Linagliptin inhibits FAP with an IC50 of 89 nM (approximately 90-fold selectivity versus DPP-4)[2] |
| 细胞实验 | In male Wistar rats， Beagle dogs， and Rhesus monkeys， xanthine linagliptin proves to be a highly efficacious， long-lasting， and potent DPP-4 inhibitor providing >70% inhibition for >7 h for all three species after oral administration of 1 mg/kg. Single oral administration of linagliptin to db/db mice 45 min prior to an oral glucose tolerance test reduced plasma glucose excursion in a dose-dependent manner from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition)[1]. Linagliptin (3 and 10 mg/kg) dose-dependently inhibits the DPP-4 enzyme in plasma within 30 min of administration. Linagliptin (1 mg/kg， p.o.) significantly reduces glucose excursion by approximately 50%[2]. Oral administration of the DPP-4 inhibitor linagliptin (3 mg/kg， p.o.) strongly reduces DPP-4 activity， stabilizes active GLP-1 in chronic wounds， and improves healing in ob/ob mice. At day 10 postwounding， linagliptin-treated ob/ob mice show largely epithelialized wounds characterized by the absence of neutrophils[3]. |
| 细胞实验 | A total of 4.0×107 keratinocytes per well are seeded into 24-well plates. After reaching 50% confluence， cells are starved for 24 h with DMEM. Proliferation of cells is assessed by using 1 μCi/mL of [3H]methyl-thymidine in DMEM in the presence of 10% fetal bovine serum and increasing concentrations of linagliptin (3， 30， 300， or 600 nM) for 24 h. Cells are then washed twice with phosphate-buffered saline and incubated in 5% trichloroacetic acid at 4°C for 30 min， and the DNA is solubilized in 0.5mol/LNaOH for 30 min at 37°C. Finally， [3H]thymidine incorporation is determined.[1-4] |
| 动物实验 | Each experimental group (vehicle or linagliptin treatment) consists of 10 individual ob/ob mice (n=10). Animals are treated orally once a day (8:00 AM) by gastrogavage using vehicle (1% methylcellulose) or linagliptin (3 mg/kg body weight in 1% methylcellulose) beginning 2 days (day?2) before wounding. After wounding， animals are subsequently treated once a day throughout the 10-day healing period.[1-4] |
| 激酶实验 | EDTA plasma (20 μL) is diluted with 30 μL of DPP-4 assay buffer (100 mM Tris and 100 mM NaCl， adjusted to pH 7.8 with HCl) and mixed with 50 μL of H-Ala-Pro-7-amido-4-trifluoromethylcoumarin. The 200 mM stock solution in dimethylformamide is diluted 1:1000 with water to yield a final concentration of 100 μM. The plate is incubated at room temperature for 10 min， and fluorescence in the wells is determined by using a Victor 1420 Multilabel Counter at an excitation wavelength of 405 nm and an emission wavelength of 535 nm. For the detection of DPP-4 activity in wound lysates， 100 μg of protein from the respective wound lysates are used instead of 20 μL of plasma. Active GLP-1 is also detected from 100 μg of respective wound tissue samples and analyzed by using the Mouse/Rat Total Active GLP-1 Assay Kit.[1-4] |
| 数据来源文献 | [1]. Eckhardt M， 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 d [2]. Thomas L， et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-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 [3]. Schurmann C， et al. The dipeptidyl peptidase-4 inhibitor linagliptin attenuates inflammation and accelerates epithelialization in wounds of diabetic ob/ob mice. J Pharmacol Exp Ther. 2012 Jul;342(1):71-80. [4]. Huan Y， et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7(1):4351. |
| 单位 | 瓶 |
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