Rivaroxaban (Xarelto; BAY 59-7939) is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders. Rivaroxaban (Xarelto; BAY 59-7939) inhibits clot-associated,free
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Coagulation factor X inhibitor
Product Description
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.
1.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, [PMID:][10.1080/00032719.2022.2053700]
2.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]
3.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]
4.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]
5.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]
References
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][10.1021/op500134e]
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][10.1021/op500134e]
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, [PMID:][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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