Description
INTRODUTION
Apixaban is a highly selective, reversible, and direct inhibitor of Human Factor X and Rabbit Factor X with Ki of 0.08 nM and 0.17 nM, respectively. Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor X with Ki of 0.08 nM and 0.17 nM for Human Factor X and Rabbit Factor X, respectively. In vitro, Apixaban prolongs the clotting times of normal human plasma with theconcentrations (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 highestpotency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays.
Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development
USAGE
Apixaban is a highly selective, reversible, and direct inhibitor of Human Factor X and Rabbit Factor X with Ki of 0.08 nM and 0.17 nM, respectively. Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor X with Ki of 0.08 nM and 0.17 nM for Human Factor X and Rabbit Factor X, respectively. In vitro, Apixaban prolongs the clotting times of normal human plasma with theconcentrations (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 highestpotency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays.
Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development
USAGE
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| Product name | Apixaban | |
| Items | Standards | Results |
| Appearance | White to off-white solid powder | Complies |
| Identification | By HNMR | Complies |
| By HPLC | Complies | |
| Loss on Drying | ≤ 0.50% | 0.10% |
| Heavy Metals | ≤ 20ppm | Complies |
| Residue on Ignition | ≤ 0.10% | 0.08% |
| Related Substances | Any single impurity: ≤0.10% | 0.05% |
| Total impurities: ≤0.50% | 0.10% | |
| HPLC | ≥ 99.5% | 99.90% |
| Assay(HPLC basis on drying) | 98.0%~102.0% | 99.88% |
| Reference Standard | In-house Standard | |
| Conclusion | The product complied to In-house standard. | |
| Storage | Preserve in tight,light-resistant containers in a cool place | |
