Linagliptin (BI-1356)
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.
BI1356是一种有效的DPP-4竞争性抑制剂,在多个独立的DPP-4抑制活性实验中得到的IC50值为0.4、0.5、0.9和1.1 nM。
DPP-4是一种N端二肽基肽酶,是膜结合蛋白,也是血浆中的可溶性蛋白。该物质在肠促胰岛素的降解中具有重要作用,如GLP-1,其在葡萄糖代谢过程中相当重要。在生理学条件下,位于毛细血管内皮靠近L细胞的DPP-4可将分泌到回肠的GLP-1快速截断。GLP-1可使β-细胞对葡萄糖刺激敏感,进而提高β-细胞的胞内cAMP浓度,加速并增强葡萄糖吸收的胰岛素响应。通过对底物结合位点的测试,BI1356抑制DPP-4酶。[1]
从融合Caco-2细胞中提取DPP-4,以测定BI1356的抑制活性。通过混合抑制剂溶液和底物及Caco-2细胞提取物进行实验,结果表明BI1356抑制DPP-4的IC50值为0.4、0.5、0.9和1.1 nM。相比其他二肽基肽酶氨肽酶N和P、脯氨酰寡肽酶和诸如胰蛋白酶、纤溶酶和凝血酶的蛋白酶,BI1356具有非常显著的DPP-4选择性。[1]
体内实验表明,BI1356给药30 min后可剂量依赖地抑制血浆中的DPP-4酶。从1到10 mg/kg不等的剂量表现出了显著的DPP-4抑制活性,并表现出持续的DPP-4抑制活性。给药后24 h抑制血浆DPP-4活性的ED50值为0.9 mg/kg。在临床研究中,BI1356显著而持续地改善了血糖控制能力,在临床上具有重要意义,并同时提高了β-细胞的功能参数。使用BI1356的病人似乎相对于对照组呈现≥ 0.5%的HbA1c下降。[1,2]
参考文献:
1. Thomas L, Eckhardt M, Langkopf E, 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 compared with other dipeptidyl peptidase-4 inhibitors[J]. Journal of Pharmacology and Experimental Therapeutics, 2008, 325(1): 175-182.
2. Del Prato S, Barnett A H, Huisman H, et al. Effect of linagliptin monotherapy on glycaemic control and markers of β‐cell function in patients with inadequately controlled type 2 diabetes: a randomized controlled trial[J]. Diabetes, Obesity and Metabolism, 2011, 13(3): 258-267.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 472.5 |
Cas No. | 668270-12-0 |
Formula | C25H28N8O2 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥17.85 mg/mL in DMSO |
Chemical Name | 8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione |
SDF | Download SDF |
Canonical SMILES | CC#CCN1C2=C(N=C1N3CCCC(C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C |
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 | Linagliptin是一种高度有效的二肽基肽酶4(DDP-4)竞争性抑制剂,IC50值为1 nM。 | |||||
靶点 | DDP-4 | |||||
IC50 | 1 nM |
质量控制和MSDS
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