Online Exporter Doxycycline Hyclate 150 Mg - Apixaban – CPF

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Background

Apixaban is a highly selective and reversible inhibitor of Factor Xa with Ki values of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].

Factor X, also known by the eponym Stuart–Prower factor, is an enzyme of the coagulation cascade. Factor X is activated, by hydrolysis, into factor Xa by both factor IX. Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa could offer an alternate method for anticoagulation. Direct Xa inhibitors are popular anticoagulants [2].

In vitro: Apixabanhas exhibited 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 [1]. Apixaban prolonged the clotting times of normal human plasma with the concentrations (EC2x) of 3.6, 0.37, 7.4 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 showed the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays [3].

In vivo: Apixaban exihibited the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1h-1), and low volume of distribution (Vdss: 0.2 L/kg) in the dog. Besides, Apixaban also showed a moderate half-life with T1/2 of 5.8 hours and good oral bioavailability (F: 58%) [1]. In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produced antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM in a dose-dependent manner[3]. Apixaban significantly inhibited factor Xa activity with an IC50 of 0.22 μM in rabbit ex vivo[4]. In chimpanzee, Apixaban also showed small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1h-1), and good oral bioavailability (F: 59%) [5].

References:
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 antihemostaticstudies[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.

Apixaban is a highly selective and reversible inhibitor of Factor Xa with Ki values of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].

Factor X, also known by the eponym Stuart–Prower factor, is an enzyme of the coagulation cascade. Factor X is activated, by hydrolysis, into factor Xa by both factor IX. Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa could offer an alternate method for anticoagulation. Direct Xa inhibitors are popular anticoagulants [2].

In vitro: Apixabanhas exhibited 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 [1]. Apixaban prolonged the clotting times of normal human plasma with the concentrations (EC2x) of 3.6, 0.37, 7.4 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 showed the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays [3].

In vivo: Apixaban exihibited the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1h-1), and low volume of distribution (Vdss: 0.2 L/kg) in the dog. Besides, Apixaban also showed a moderate half-life with T1/2 of 5.8 hours and good oral bioavailability (F: 58%) [1]. In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produced antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM in a dose-dependent manner[3]. Apixaban significantly inhibited factor Xa activity with an IC50 of 0.22 μM in rabbit ex vivo[4]. In chimpanzee, Apixaban also showed small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1h-1), and good oral bioavailability (F: 59%) [5].

References:
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 antihemostaticstudies[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.

Chemical structure

Apixaban

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

OUR STRENGTH

Quality management1

Proposal 18 Quality Consistency Evaluation projects which have approved 4, and 6 projects are under approving.

Quality management2

Advanced international quality management system has laid solid foundation for sales.

Quality management3

Quality supervision runs through the whole life cycle of the product to ensure the quality and therapeutic effect. 

Quality management4

Professional Regulatory Affairs team supports the quality demands during the application and registration.


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As for aggressive rates, we believe that you will be searching far and wide for anything that can beat us. We can easily state with absolute certainty that for such good quality at such charges we are the lowest around for Online Exporter Doxycycline Hyclate 150 Mg - Apixaban – CPF , The product will supply to all over the world, such as: Swaziland, Peru, El Salvador, In order to meet more market demands and long-term development, a 150, 000-square-meter new factory is under construction, which will be put into use in 2014. Then, we shall own a large capacity of producing. Of course, we are going to continue improving the service system to meet the requirements of customers, bringing health, happiness and beauty to everyone.
  • The factory can meet continuously developing economic and market needs, so that their products are widely recognized and trusted, and that's why we chose this company.
    5 Stars By Antonio from Johannesburg - 2017.01.28 18:53
    The factory workers have a good team spirit, so we received high quality products fast, in addition, the price is also appropriate, this is a very good and reliable Chinese manufacturers.
    5 Stars By Sahid Ruvalcaba from Germany - 2018.05.13 17:00
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