Rivaroxaban D4
(Synonyms: 5-氯-N-[[(5S)-2-氧代-3-[4-(3-氧代-4-吗啉基)苯基-2,3,5,6-D4]-5-恶唑烷基]甲基]-2-噻吩甲酰胺,BAY 59-7939-d4) 目录号 : GC60326
An internal standard for the quantification of rivaroxaban
Cas No.:1132681-38-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rivaroxaban-d4 is intended for use as an internal standard for the quantification of rivaroxaban by GC- or LC-MS. Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.1 It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases. In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time. Formulations containing rivaroxaban have been used as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.2,3
1.Turpie, A.G.G.Oral, direct factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseasesArterioscler. Thromb. Vasc. Biol.27(6)1238-1247(2007) 2.Babilonia, K., and Trujillo, T.The role of prothrombin complex concentrates in reversal of target specific anticoagulantsThromb. J.12:8(2014) 3.Turpie, A.G.G.Rivaroxaban as an oral anticoagulant for stroke prevention in atrial fibrillationTher. Clin. Risk Manag.10197-205(2014)
| Cas No. | 1132681-38-9 | SDF | |
| 别名 | 5-氯-N-[[(5S)-2-氧代-3-[4-(3-氧代-4-吗啉基)苯基-2,3,5,6-D4]-5-恶唑烷基]甲基]-2-噻吩甲酰胺,BAY 59-7939-d4 | ||
| Canonical SMILES | O=C(C1=CC=C(Cl)S1)NC[C@H]2CN(C3=C([2H])C([2H])=C(N4C(COCC4)=O)C([2H])=C3[2H])C(O2)=O | ||
| 分子式 | C19H14D4ClN3O5S | 分子量 | 439.91 |
| 溶解度 | DMSO : 50 mg/mL (113.66 mM; Need ultrasonic) | 储存条件 | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2732 mL | 11.366 mL | 22.7319 mL |
| 5 mM | 0.4546 mL | 2.2732 mL | 4.5464 mL |
| 10 mM | 0.2273 mL | 1.1366 mL | 2.2732 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Liquid chromatography-tandem mass spectrometry method for determination of rivaroxaban in human plasma and its application to a pharmacokinetic study
Eur J Mass Spectrom (Chichester) 2020 Apr;26(2):91-105.PMID:31514543DOI:10.1177/1469066719875014.
A high-performance liquid chromatography tandem mass spectrometric method for the determination of Rivaroxaban in human plasma has been developed and validated using Rivaroxaban D4 as an internal standard. The extraction of analyte and internal standard was accomplished by solid phase extraction technique. The method has been validated over a concentration range of 5.96-801 ng/mL. Chromatographic separations were achieved using Gemini C18, 150 mm × 4.6 mm, 5 µm, column eluted at flow rate of 1.5 mL/min with mobile phase (acetonitrile: ammonium acetate buffer (80:20 v/v)). The overall run time of method was about 1.8 min with elution times of Rivaroxaban and its internal standard Rivaroxaban D4 at around 1.18 min. The multiple reaction monitoring transitions were set at 436/145 (m/z) and 440/145 (m/z) for Rivaroxaban and Rivaroxaban D4, respectively. The calibration curves were linear (r2 ≥ 0.99) over the range of 5.96-801 ng/mL with lower limit of quantitation validated at 5.96 ng/mL. Extraction recoveries were >88% for both rivaroxaban and its stable labeled internal standard Rivaroxaban D4. The inter-day/between run precisions were ranged from 1.08% to 3.75%, while accuracy ranged from 96.3% to 102%. The presented method was used in pharmacokinetic study in healthy volunteers. Results of incurred sample reanalysis were within the acceptance range of ±20% of original value, for 98.3% of samples reanalyzed. This indicated good assay precision of target analytes in their real matrix at the employed experimental conditions. The applicability of the assay for the determination of the pharmacokinetic parameters was demonstrated.