| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A409187-1ml |
1ml |
现货  |
|
| 别名 | 阿哌沙班（BMS 562247-01） |
|---|---|
| 英文别名 | 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Apixaban (BMS 562247-01) |
| 生化机理 | 阿哌沙班（BMS 562247-01）是一种高选择性、可逆的 Xa 因子抑制剂，在人和兔体内的Ki值分别为 0.08 nM 和 0.17 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 凝血因子 X 抑制剂 |
| 产品介绍 |
Apixaban是一种高度选择性，可逆的凝血因子 Xa 抑制剂，抑制人和兔凝血因子 Xa 的 Ki 值分别为 0.08 nM 和 0.17 nM。Apixaban 正在开发用于预防和治疗各种血栓栓塞疾病。 Information Apixaban (BMS 562247-01) Apixaban (BMS 562247-01) is a highly selective, reversible inhibitor of Factor Xa with K i of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor Xa with Ki of 0.08 nM and 0.17 nM for Human Factor Xa and Rabbit Factor Xa, respectively. In vitro, Apixaban prolongs the clotting times of normal human plasma with the concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays. In vivo In the dog, Apixaban shows the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1 h-1), and low volume of distribution (Vdss: 0.2 L kg-1). Besides, Apixaban also exhibits a moderate half-life (T1/2: 5.8 hours) and good oral bioavailability (F: 58%). In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produces dose-dependent antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM, respectively. Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo. In chimpanzee, Apixaban also shows small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1 h-1), and good oral bioavailability (F: 59%). cell lines：MDA-MB-231 breast cancer and SK-OV-3 ovarian cancer cell lines Concentrations： Incubation Time： Powder Purity:≥95% |
| ALogP | 2.865 |
|---|---|
| hba_count | 5 |
| HBD Count | 1 |
| Rotatable Bond | 5 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=CC=C(C=C1)[N]2N=C(C(N)=O)C3=C2C(=O)N(CC3)C4=CC=C(C=C4)N5CCCCC5=O |
| 分子量 | 459.5 |
| Reaxy-Rn | 11244786 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11244786&ln= |
| DMSO(mg / mL) Max Solubility | 18 |
|---|---|
| DMSO(mM) Max Solubility | 39.17 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 11244786 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11244786&ln= |
| Concentration(Compounding value) | 9-11（mmol/L） |
|---|---|
| Appearance(A409187) | Colorless Transparent Liquid |
| Record the entire process by video | Conform |
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