Apixaban NEW
| Price | $33 | $45 | $54 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Apixaban | CAS No.: 503612-47-3 |
| Purity: 100% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Apixaban |
| Description | Apixaban (BMS-562247-01) is an orally active anticoagulant that inhibits coagulation factor Xa, directly preventing the conversion of prothrombin to thrombin and the formation of cross-linked fibrin clots. |
| Kinase Assay | Purified FXa is obtained after activation with Russell's viper venom followed by affinity chromatography. The resulting FXa is > 95% pure as judged by sodium dodecylsulfate polyacrylamide gel electrophoresis. The substrate affinity values for FXa, expressed as the Michaelis-Menten-Henri constant (Km), for human, rabbit, rat and dog FXa are determined using the chromogenic substrate S-2765, and are 36, 60, 240 and 70 μM, respectively. The substrate hydrolysis is monitored by measuring absorbance at 405 nm at 25°C for up to 30 min using a SpectraMax 384 Plus plate reader and SoftMax. FXa activity for each substrate and inhibitor concentration pair is determined in duplicate. The Ki values are calculated by non-linear least-squares fitting of the steady-state substrate hydrolysis rates to the equation for competitive inhibition (Equation 1) using GRAFIT, where v equals reactions velocity in OD min?1, Vmax equals maxiumum reaction velocity, S equals substrate concentration, and I equals inhibitor concentration. |
| In vitro | Apixaban demonstrates excellent pharmacokinetic properties in dogs, characterized by very low clearance (Cl: 0.02 L/kg/h), low volume of distribution (Vdss: 0.2 L/kg), a half-life (T1/2: 5.8 h), and oral bioavailability (F: 58%). Its antithrombotic efficacy is evident in models of venous thrombosis, arteriovenous shunt thrombosis, and electrically induced carotid artery thrombosis in rabbits, with EC50 values of 110 nM, 270 nM, and 70 nM, respectively. |
| In vivo | When applied to normal human plasma in vitro, Apixaban extends coagulation time, doubling the prothrombin time (3.6 μM), modified prothrombin time (0.37 μM), activated partial thromboplastin time (7.4 μM), and HepTest (0.4 μM). Apixaban exhibits high selectivity in inhibiting human and rabbit Factor Xa, with Ki values of 0.08 and 0.17 nM, respectively. Additionally, Apixaban demonstrates maximum effectiveness in human and rabbit plasma in PT (Prothrombin Time) and APTT (Activated Partial Thromboplastin Time) assays, with comparatively lesser effects observed in rat and dog plasma. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 4.59 mg/mL (10 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | Fxa | Inhibitor | rabbit | Factor Xa | clotting | Factor | plasma | human | EC2x | Apixaban | inhibit |
| Inhibitors Related | Edoxaban | Heparin sodium salt | 2-Methoxyphenothiazine | Coumarin |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Address: 36?Washington?Street, Wellesley?Hills
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