BIBR-1048
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.
Dabigatran etexilate(BIBR-1048)是凝血酶的强效选择性和竞争性抑制剂。它是dabigatran的口服前体药物。针对人凝血酶的Ki值为4.5 nM,针对凝血酶诱导的血小板聚集IC50为10 nM[1,2]。
凝血酶是凝血因子II水解得到的蛋白,是凝血级联中的初始步骤。它把纤维蛋白原转变成纤维蛋白,激活其他因子,在血液内稳态、伤口愈合和炎症中发挥重要作用。
在体外,dabigatran显示出抗凝血作用,具有一定的浓度依赖性。在人PPP中,它将活化部分促凝血酶原激酶时间、凝血酶原时间及静脉酶凝结时间增加了一倍[1]。
在大鼠和猕猴中,dabigaran延长了活化部分凝血酶的时间。大鼠口服给药dabigatran etexilate以时间和剂量依赖性的方式产生抗凝作用[1]。 在心房颤动的患者中,与warfarin相比,口服dabigatran 150 mg,中风和全身性栓塞的速度明显下降,但出血率没有明显变化[2]。
参考文献:
1. Wienen W, Stassen JM, Priepke H et al. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.
2. Connolly SJ, Ezekowitz MD, Yusuf S et al. Dabigatran versus warfarin in patients with atrial fibrillation. N Engl J Med. 2009 Sep 17;361(12):1139-51.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 627.73 |
Cas No. | 211915-06-9 |
Formula | C34H41N7O5 |
Solubility | ≥30 mg/mL in DMSO; insoluble in H2O; ≥22.13 mg/mL in EtOH |
Chemical Name | ethyl 3-[[2-[[4-[(Z)-N'-hexoxycarbonylcarbamimidoyl]anilino]methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoate |
SDF | Download SDF |
Canonical SMILES | CCCCCCOC(=O)N=C(C1=CC=C(C=C1)NCC2=NC3=C(N2C)C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4)N |
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。 |
质量控制和MSDS
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