| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 2mg | |||
| Other Sizes |
| Targets |
Factor Xa (F10). Apixaban 13CD3 selectively and reversibly inhibits free and prothrombinase-bound factor Xa, which plays a central role in the coagulation cascade by converting prothrombin to thrombin. Inhibition of factor Xa reduces thrombin generation, thereby decreasing fibrin clot formation and platelet aggregation.
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|---|---|
| ln Vitro |
Apixaban inhibits human factor Xa with a Ki of 0.08 nM. It shows similar potency against rabbit factor Xa (Ki = 0.17 nM). The compound is highly selective for factor Xa over other serine proteases, including thrombin, trypsin, plasmin, and tissue-type plasminogen activator (IC50 > 20 microM).
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| ln Vivo |
In a rabbit model of venous thrombosis, oral administration of apixaban (0.3-3 mg/kg) produces dose-dependent antithrombotic effects, including inhibition of clot formation and reduction of thrombus weight. The ED50 for antithrombotic effect is approximately 1.5 mg/kg. These in vivo antithrombotic effects are consistent with its potent factor Xa inhibition profile.
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| Enzyme Assay |
Radioligand binding assays are performed using purified human factor Xa. Varying concentrations of apixaban 13CD3 are incubated with factor Xa (0.1-0.5 nM) and a fluorogenic substrate (e.g., methoxycarbonyl-cyclohexylglycyl-glycyl-arginine-AMC acetate) in Tris buffer. The rate of substrate hydrolysis is measured by fluorescence (excitation at 360 nm, emission at 460 nm) over 10-20 minutes. Ki values are calculated from dose-response curves using enzyme kinetic models.
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| Cell Assay |
Not applicable, as apixaban acts directly on a purified plasma coagulation factor rather than through a cellular target. In vitro assays are typically cell-free enzyme activity assays. For cellular assays, human whole blood or platelet-rich plasma may be used to measure clotting times (PT, aPTT) using a coagulometer after addition of the test compound.
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| Animal Protocol |
Male New Zealand White rabbits (2.5-3.5 kg) are anesthetized, and the jugular vein is isolated. A segment of the vein is isolated between two ligatures, and 0.1 mL of bovine thromboplastin is injected into the isolated segment. Five minutes later, a silk thread pre-wetted with a standardized thrombogenic solution is inserted, and the segment is closed. After 20 minutes, the thrombus formed on the thread is weighed. Apixaban is administered orally 30 minutes prior to the thrombus induction.
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| ADME/Pharmacokinetics |
Apixaban 13CD3 serves as an internal standard for LC-MS/MS quantification of apixaban. The parent drug apixaban is orally bioavailable (~50-66%) with a half-life of approximately 12 hours in humans. It is rapidly absorbed (Tmax ~3-4 hours), and ~87% is protein bound (primarily to albumin). Apixaban is metabolized primarily by CYP3A4 and excreted via both renal and biliary routes.
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| Toxicity/Toxicokinetics |
Apixaban is generally well tolerated, with bleeding being the primary adverse effect. In clinical trials, the incidence of major bleeding was approximately 2-3% in patients receiving apixaban. The most common bleeding events include epistaxis, gastrointestinal bleeding, and bruising. Other side effects include nausea, anemia, and thrombocytopenia. Apixaban 13CD3 is not for therapeutic use.
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| References | |
| Additional Infomation |
Apixaban was approved by the FDA in 2012 for the reduction of stroke and systemic embolism in non-valvular atrial fibrillation, and for the treatment and prevention of deep vein thrombosis (DVT) and pulmonary embolism (PE). It is marketed under the brand name Eliquis®. The 13CD3-labeled version is exclusively a research internal standard for precise drug quantification in biological matrices.
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| Molecular Formula |
C2413CH22D3N5O4
|
|---|---|
| Molecular Weight |
463.508245229721
|
| Exact Mass |
463.212
|
| CAS # |
1261393-15-0
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| Related CAS # |
Apixaban;503612-47-3
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| PubChem CID |
49849553
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.705
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
34
|
| Complexity |
777
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[2H][13C]([2H])([2H])OC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)N
|
| InChi Key |
QNZCBYKSOIHPEH-KQORAOOSSA-N
|
| InChi Code |
InChI=1S/C25H25N5O4/c1-34-19-11-9-18(10-12-19)30-23-20(22(27-30)24(26)32)13-15-29(25(23)33)17-7-5-16(6-8-17)28-14-3-2-4-21(28)31/h5-12H,2-4,13-15H2,1H3,(H2,26,32)/i1+1D3
|
| Chemical Name |
7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-1-[4-(trideuterio(113C)methoxy)phenyl]-4,5-dihydropyrazolo[3,4-c]pyridine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5.56 mg/mL (~12.00 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (1.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.56 mg/mL (1.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.56 mg/mL (1.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1575 mL | 10.7873 mL | 21.5745 mL | |
| 5 mM | 0.4315 mL | 2.1575 mL | 4.3149 mL | |
| 10 mM | 0.2157 mL | 1.0787 mL | 2.1575 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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