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利伐沙班, 凝血因子 X 抑制剂

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货号 (SKU) 包装规格 是否现货 价格 数量
R125138-10mg
 10mg 现货 Stock Image
R125138-50mg
 50mg 现货 Stock Image
R125138-250mg
 250mg 现货 Stock Image
R125138-1g
 1g 现货 Stock Image
R125138-5g
 5g 现货 Stock Image
R125138-25g
 25g 现货 Stock Image
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Amino Acid/Protein Metabolism (4559) coagulation factor X Inhibitor (9) Factor Xa (34) Metabolic Enzyme/Protease (4889)
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基本描述

别名 利伐沙班
英文别名 B01AF01 | 1429742-50-6 | 2-Thiophenecarboxamide, 5-chloro-N-(((5S)-2-oxo-3-(4-(3-oxo-4-morpholinyl)phenyl)-5-oxazolidinyl)methyl)- | 2w26 | 9NDF7JZ4M3 | Q420262 | Xarelto | MFCD11974010 | N-Smc-carboxylate | L-Glutatione | RIVAROXABAN [ORANGE BOOK] | MLS0
规格或纯度 Moligand™, ≥99%
英文名称 Rivaroxaban
生化机理 利伐沙班（Xarelto；BAY 59-7939）是一种新型口服直接因子 Xa（FXa）抑制剂，目前正处于后期开发阶段，用于预防和治疗血栓栓塞性疾病。利伐沙班（Xarelto；BAY 59-7939）可抑制血栓相关的游离 FXa 活性和凝血酶原酶活性，此外，它还能减少凝血酶的生成。利伐沙班（Xarelto; BAY 59-7939）是一种有效的抗血栓药物。
储存温度 -20°C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.

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 drug transport up to concentrations of 100 μM in vitro.
纯度 ≥99%

产品属性

ALogP 2.5

关联靶点（人）

F10 Tclin 凝血因子 X(Coagulation factor X) (20 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
F2 Tclin Thrombin (11687 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PGR Tclin Progesterone receptor (8562 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RARA Tclin Retinoic acid receptor alpha (1324 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PPARA Tclin Peroxisome proliferator-activated receptor alpha (9197 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
F10 Tclin Coagulation factor X (9693 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RARG Tclin Retinoic acid receptor gamma (1154 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RARB Tclin Retinoic acid receptor beta (1232 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDE4A Tclin Phosphodiesterase 4A (1943 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MC3R Tchem Melanocortin receptor 3 (5659 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR1H4 Tclin Bile acid receptor FXR (6228 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR1H3 Tchem LXR-alpha (2891 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Trypsin (394 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Oryctolagus cuniculus (11301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
H9c2 (3506 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Blood (6 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504765023
EC号 685-132-2
分子类型 小分子
IIUPAC Name 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
INCHI 1S/C19H18ClN3O5S/c20-16-6-5-15(29-16)18(25)21-9-14-10-23(19(26)28-14)13-3-1-12(2-4-13)22-7-8-27-11-17(22)24/h1-6,14H,7-11H2,(H,21,25)/t14-/m0/s1
InChi Key KGFYHTZWPPHNLQ-AWEZNQCLSA-N
Smiles C1COCC(=O)N1C2=CC=C(C=C2)N3CC(OC3=O)CNC(=O)C4=CC=C(S4)Cl
Isomeric SMILES C1COCC(=O)N1C2=CC=C(C=C2)N3C[C@@H](OC3=O)CNC(=O)C4=CC=C(S4)Cl
关联CAS 366789-02-8
PubChem CID 9875401
MeSH Entry Terms 5-chloro-N-(((5S)-2-oxo-3-(4-(3-oxomorpholin-4-yl)phenyl)-1,3-oxazolidin-5-yl)methyl)thiophene-2-carboxamide;BAY 59 7939;BAY 59-7939;BAY 597939;rivaroxaban;xarelto
分子量 435.88

化学和物理性质

溶解性 DMSO 87 mg/mL Ethanol <1 mg/mL
比旋光度 [α]/D -34 to -44, c = 0.3 in DMSO
熔点 230 °C
分子量 435.900 g/mol
XLogP3 2.500
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 435.066 Da
单同位素质量Monoisotopic Mass 435.066 Da
拓扑极表面积Topological Polar Surface Area 116.000 Ų
重原子数Heavy Atom Count 29
形式电荷Formal Charge 0
复杂度Complexity 645.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 1
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性（GHS）

象形图 GHS09
信号词 Warning
危险声明

H411: 对水生生物有毒并具有长期持续影响
预防措施声明

P273: 避免释放到环境中。

P391: 收集溢出物

P501: 将内容物/容器处理到。。。

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批号(Lot Number) 证书类型 货号
B2021072 分析证书 R125138
L2420117 分析证书 R125138
I2226099 分析证书 R125138
F2214241 分析证书 R125138
F2214248 分析证书 R125138
K2125024 分析证书 R125138
K2125025 分析证书 R125138
K2125026 分析证书 R125138
K2125170 分析证书 R125138
K2125022 分析证书 R125138
D2121060 分析证书 R125138
E1522122 分析证书 R125138
I2226096 分析证书 R125138
I2226097 分析证书 R125138
I2226098 分析证书 R125138
I2226100 分析证书 R125138
E2424015 分析证书 R125138

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引用文献

1. Bosch J, Eikelboom JW, Connolly SJ, Bruns NC, Lanius V, Yuan F, Misselwitz F, Chen E, Diaz R, Alings M et al..  (2017)  Rationale, Design and Baseline Characteristics of Participants in the Cardiovascular Outcomes for People Using Anticoagulation Strategies (COMPASS) Trial..  Can J Cardiol,  33  (8): (1027-1035).  [PMID:28754388]
2. Anand SS, Bosch J, Eikelboom JW, Connolly SJ, Diaz R, Widimsky P, Aboyans V, Alings M, Kakkar AK, Keltai K et al..  (2018)  Rivaroxaban with or without aspirin in patients with stable peripheral or carotid artery disease: an international, randomised, double-blind, placebo-controlled trial..  Lancet,  391  (10117): (219-229).  [PMID:29132880]
3. Ru Li, Xuan Zou, Pan Luan, Xiaokun Liu, Ning Wang, Qian Wang, Huashi Guan, Zhe Xu.  (2022)  Direct Determination of Enzymes in Dried Blood Spots by High-Performance Liquid Chromatography – Mass Spectrometry (HPLC-MS) for the Screening of Antithrombotic Agents.  ANALYTICAL LETTERS,  [10.1080/00032719.2022.2053700]
4. Xu Wang, Dai-Yan Zhang, Shi-Jun Yin, Hui Jiang, Min Lu, Feng-Qing Yang, Yuan-Jia Hu.  (2021)  Screening of Potential Thrombin and Factor Xa Inhibitors from the Danshen–Chuanxiong Herbal Pair through a Spectrum–Effect Relationship Analysis.  MOLECULES,  26  (23): (7293).  [PMID:34885877] [10.3390/molecules26237293]
5. Yang Yi-Yao, Wu Zhao-Yu, Xia Fang-Bo, Zhang Hao, Wang Xu, Gao Jian-Li, Yang Feng-Qing, Wan Jian-Bo.  (2020)  Characterization of thrombin/factor Xa inhibitors in Rhizoma Chuanxiong through UPLC-MS-based multivariate statistical analysis.  Chinese Medicine,  15  (1): (1-14).  [PMID:32874198] [10.1186/s13020-020-00376-0]
6. Yang Yi-Yao, Wu Zhao-Yu, Zhang Hao, Yin Shi-Jun, Xia Fang-Bo, Zhang Qian, Wan Jian-Bo, Gao Jian-Li, Yang Feng-Qing.  (2020)  LC–MS-based multivariate statistical analysis for the screening of potential thrombin/factor Xa inhibitors from Radix Salvia Miltiorrhiza.  Chinese Medicine,  15  (1): (1-13).  [PMID:32351617] [10.1186/s13020-020-00320-2]
7. Zhe Xu, Ruonan Liu, Huashi Guan.  (2017)  Dual-target inhibitor screening against thrombin and factor Xa simultaneously by mass spectrometry.  ANALYTICA CHIMICA ACTA,  990  (1).  [PMID:29029731] [10.1016/j.aca.2017.07.063]

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