Apixaban
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.
Apixaban是一种高选择性、可逆的Factor Xa抑制剂,在人和兔中的Ki分别为0.08 nM和0.17 nM [1]。
Factor Xa,也称为Stuart-Prower因子,是凝血级联的酶。Factor X被Factor IX水解活化为Factor Xa。Factor Xa是凝血因子血栓激酶的活化形式。抑制Factor Xa将提供抗凝的替代方法。针对Factor Xa的抑制剂是流行的抗凝剂[2]。
体外实验:Apixaban对Factor Xa表现出高度的效力、选择性和功效,对人Factor Xa和兔Factor Xa的Ki分别为0.08 nM和0.17 nM [1]。3.6 μM、0.37 μM、7.4 μM和0.4 μM的浓度(EC2x)的Apixaban延长正常人血浆的凝血时间,这些浓度分别是使凝血酶原时间(PT)、修饰凝血酶原时间(mPT)、激活部分凝血活酶时间(APTT)和HepTest加倍所需的浓度。此外,Apixaban在人和兔血浆中显示出最高的效力,在大鼠和狗血浆中, PT和APTT测定中的效力较低[3]。
在体实验:Apixaban在狗中以非常低的清除率(Cl:0.02L kg-1h-1)和低体积分布(Vdss:0.2L kg-1)显示出优异的药代动力学。此外,Apixaban也表现出适度的半衰期,T1/2为5.8小时,口服生物利用度良好(F:58%)[1]。在动静脉分流血栓形成(AVST)、静脉血栓形成(VT)和电介导的颈动脉血栓形成(ECAT)兔模型中,Apixaban以剂量依赖性方式产生抗血栓形成效应,EC50分别为270 nM、110 nM和70 nM [3 ]。Apixaban显著抑制Factor Xa的活性,兔体外IC50为0.22 μM[4]。在黑猩猩中,Apixaban具有较小体积分布(Vdss:0.17 L/kg)、低全身清除率(Cl:0.018L kg-1h-1)和良好的口服生物利用度(F:59%)[5]。
参考文献:
Pinto D J P, Orwat M J, Koch S, et al. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl) phenyl)-4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4-c] pyridine-3-carboxamide (Apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa[J]. Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors as Anticoagulants[J].
Wong P C, Crain E J, Xin B, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies[J]. Journal of Thrombosis and Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits[J]. Journal of thrombosis and thrombolysis, 2010, 29(1): 70-80.
He K, Luettgen J M, Zhang D, et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor[J]. European journal of drug metabolism and pharmacokinetics, 2011, 36(3): 129-139.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 459.5 |
Cas No. | 503612-47-3 |
Formula | C25H25N5O4 |
Solubility | insoluble in H2O; ≥10.64 mg/mL in EtOH with gentle warming and ultrasonic; ≥11.5 mg/mL in DMSO |
Chemical Name | 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-dihydropyrazolo[3,4-c]pyridine-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | COC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)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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