| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R409000-1ml |
1ml |
现货  |
|
| 英文别名 | (S)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Rivaroxaban (BAY 59-7939) |
| 生化机理 | 利伐沙班（BAY 59-7939）是一种 Xa 因子直接抑制剂，在无细胞测定中的 Ki 和 IC50 分别为 0.4 nM 和 0.7 nM。它对人类 Xa 因子具有选择性，其选择性是其他生物相关丝氨酸蛋白酶的 10 000 倍（IC50 >20 μM）。 |
| 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 |
Rivaroxaban is an oral, direct inhibitor of Factor X, being developed for the prevention and treatment of arterial and venous thrombosis with a Ki of 0.4 nM. Rivaroxaban also inhibits prothrombinase activity (IC50 = 2.1 nM). Rivaroxaban also shows a similar affinity to purified human (IC50 = 0.7 nM) and rabbit Factor X (IC50 = 0.8 nM), but a lesser potency against purified rat Factor X (IC50 = 3.4 nM). Endogenous human and rabbit Factor X in plasma is inhibited to a similar extent by Rivaroxaban (IC50 = 21 nM and 21 nM, respectively), while 14-fold higher concentrations are required in rat plasma (IC50 = 290 nM). Rivaroxaban exhibits high permeability and polarized transport across Caco-2 cells as a substrate of the P-gp, but exhibits no inhibitory effect on P-gp-mediated drμg transport up to concentrations of 100 μM in vitro. Information Rivaroxaban (BAY 59-7939) Rivaroxaban (BAY 59-7939) is a direct inhibitor of Factor Xa with Ki and IC50 of 0.4 nM and 0.7 nM in cell-free assays, respectively. It is selective for human factor Xa, for which it has >10 000-fold greater selectivity than f Rivaroxaban is an oral, direct inhibitor of Factor Xa (FXa), being developed for the prevention and treatment of arterial and venous thrombosis with a Ki of 0.4 nM. Rivaroxaban also inhibits prothrombinase activity with IC50 of 2.1 nM. Rivaroxaban also shows a similar affinity to purified human and rabbit FXa (IC50 0.7 nM and 0.8 nM, respectively), but a lesser potency against purified rat FXa (IC50 3.4 nM). Endogenous human and rabbit FXa in plasma is inhibited to a similar extent by Rivaroxaban (IC50 21 nM and 21 nM, respectively), while 14-fold higher concentrations are required in rat plasma (IC50 290 nM). Rivaroxaban exhibits high permeability and polarized transport across Caco-2 cells as a substrate of the P-gp, but exhibits no inhibitory effect on P-gp-mediated drug transport up to concentrations of 100 μM in vitro. In vivo Rivaroxaban reduces venous thrombosis in a dose dependent manner (ED50 0.1 mg/kg i.v.) in a rat venous stasis model. Rivaroxaban reduces arterial thrombus formation in an arteriovenous (AV) shunt in rats (ED50 5.0 mg/kg p.o.) and rabbits (ED50 0.6 mg/kg p.o.). Plasma pharmacokinetics of Rivaroxaban are linear across the investigated dose range (1-10 mg/kg in rats, 0.3-3 mg/kg in dogs). Plasma clearance is low: 0.4 L/kg/h in rats and 0.3 L/kg/h in dogs; the volume of distribution (V(ss)) is moderate: 0.3 L/kg in rats, and 0.4 L/kg in dogs. The elimination half-life after oral administration is short in both species (0.9-2.3 hours). cell lines： Concentrations：0 - 100 μM Incubation Time：2 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | ClC1=CC=C(S1)C(=O)NCC2CN(C(=O)O2)C3=CC=C(C=C3)N4CCOCC4=O |
| 分子量 | 435.88 |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
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