Linagliptin NEW
| Price | $38 | $54 |
| Package | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-05 |
Product Details
| Product Name: Linagliptin | CAS No.: 668270-12-0 |
| Purity: 99.95% | Supply Ability: 10g |
| Release date: 2024/11/05 |
Product Introduction
Bioactivity
| 名稱 | Linagliptin |
| 描述 | Linagliptin (BI 1356) is a potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. |
| 細胞實驗 | 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. |
| 激酶實驗 | 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. |
| 體外活性 | Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). [1] Linagliptin acts as a competitive inhibitor with a Ki of 1 nM, and also shows 10,000-fold more selectivity for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin, and 90-fold more selectivity than fibroblast activation protein in vitro. [2] |
| 體內(nèi)活性 | In male Wistar rats, Beagle dogs, and Rhesus monkeys, Linagliptin exhibits highly efficacious, long-lasting, and potent inhibitory activity against DPP-4 with over 70% inhibition for all three species after oral administration of 1 mg/kg. In db/db mice, oral administration of Linagliptin 45 min before an oral glucose tolerance test reduces plasma glucose excursion in a dose-dependent manner, achieving 15% inhibition at 0.1 mg/kg and 66% inhibition at 1 mg/kg. [1] By inhibiting DPP-4 activity, Linagliptin also reduces the expression of the proinflammatory markers cyclooxygenase-2 and macrophage inflammatory protein-2, and enhances myofibroblast formation in healing wounds from ob/ob mice. [3] |
| 存儲條件 | keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 5.63 mg/mL (11.9 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 1 mg/mL (2.11 mM) |
| 關(guān)鍵字 | Dipeptidyl Peptidase | BI-1356 | Inhibitor | Linagliptin | BI1356 | DPP | Autophagy | Ferroptosis | inhibit |
| 相關(guān)產(chǎn)品 | Stavudine | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Paeonol | L-Cystine | Naringin | Gefitinib |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 經(jīng)典已知活性庫 | EMA 上市藥物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | FDA 上市藥物庫 | 抗癌上市藥物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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