Acenocoumarol
(Synonyms: 醋硝香豆素) 目录号 : GC32514
An anticoagulant and vitamin K antagonist
Cas No.:152-72-7
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
Acenocoumarol is an anticoagulant and vitamin K antagonist.1 It inhibits the reduction of vitamin K1 epoxide to vitamin K1 by vitamin K1 epoxide reductase (VKOR) (IC50 = 1.5 and 5.8 nM for VKORC1 and VKORC1L1, respectively).1 Acenocoumarol also inhibits a variety of VKOR mutants in cell-based reporter assays (IC50s = 0.54-11.21 nM).2 It prolongs prothrombin time in rat blood when administered at a dose of 1.5 mg/kg.3
1.Czogalla, K.J., Liphardt, K., H?ning, K., et al.VKORC1 and VKORC1L1 have distinctly different oral anticoagulant dose-response characteristics and binding sitesBlood Adv.2(6)691-702(2018) 2.Chen, X., Jin, D.-Y., Stafford, D.W., et al.Evaluation of oral anticoagulants with vitamin K epoxide reductase in its native milieuBlood132(18)1974-1984(2018) 3.Meinertz, T., Kasper, W., Kahl, C., et al.Anticoagulant activity of the enantiomers of acenocoumarolBr. J. Clin. Pharmacol.5(2)187-188(1978)
| Cas No. | 152-72-7 | SDF | |
| 别名 | 醋硝香豆素 | ||
| Canonical SMILES | O=C1C(C(C2=CC=C([N+]([O-])=O)C=C2)CC(C)=O)=C(O)C3=CC=CC=C3O1 | ||
| 分子式 | C19H15NO6 | 分子量 | 353.33 |
| 溶解度 | DMSO: 100 mg/mL (283.02 mM) | 储存条件 | Store at -20°C |
| 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 | 2.8302 mL | 14.1511 mL | 28.3022 mL |
| 5 mM | 0.566 mL | 2.8302 mL | 5.6604 mL |
| 10 mM | 0.283 mL | 1.4151 mL | 2.8302 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。
Acenocoumarol: A Review of Anticoagulant Efficacy and Safety
J Assoc Physicians India 2016 Feb;64(2):88-93.PMID:27730796doi
Anticoagulant treatment is required for the treatment and prevention of thromboembolic disorders. Vitamin K antagonists are commonly used oral anticoagulants worldwide. Acenocoumarol is mono-coumarin derivative with racemic mixture of R (+) and S (-) enantiomers. Efficacy and safety of Acenocoumarol has been evaluated in atrial fibrillation, cardiac valve replacement, after myocardial infarction, treatment of deep vein thrombosis, after major surgeries and after critical illness requiring prolonged hospitalization. Acenocoumarol is effective and safe in all age groups. It offers an advantage over warfarin in terms of better stability of anti-coagulant effect. Due to its economic advantage Acenocoumarol may be suitable oral anticoagulant for long term use in countries like India.
Biomodification of Acenocoumarol by bifidobacteria
FEMS Microbiol Lett 2021 Oct 4;368(18):fnab125.PMID:34529059DOI:10.1093/femsle/fnab125.
The increased interest of consumers in probiotic foods requires a deeper knowledge on the possible interactions with drugs, because their pharmacological properties could be modified. In this context, these studies are relevant for drugs such as Acenocoumarol, whose dosage must be controlled due to, among other factors, food-drug interactions. Acenocoumarol is an oral anticoagulant with a narrow therapeutic range. The aim of the present research is to evaluate, in vitro, the effect of bifidobacteria on Acenocoumarol. The drug was incubated with Bifidobacterium bifidum CIDCA 5310 or Bifidobacterium adolescentis CIDCA 5317 in MRS broth at 37°C for 24 h in anaerobic conditions. The effect of incubation with sterilized spent culture supernatants (SSCS) was also evaluated. Analysis by RP-HPLC showed that both bifidobacterial strains reduced the area of the Acenocoumarol peak and two new peaks were evidenced. In addition, a decrease in the intensity of the bands at 1650, 1390 and 1110/cm was observed in the FTIR spectroscopic determinations. Moreover, a new band appeared at 1720/cm. No effect on the drug was observed when incubation was performed with SSCS. The present study showed a significant change in the concentration of the anticoagulant after incubation with bifidobacteria and results are compatible with biomodification of the drug due to enzymatic activity of bifidobacteria.
Rosuvastatin-acenocoumarol interaction
Clin Ther 2005 Jun;27(6):782-4.PMID:16117985DOI:10.1016/j.clinthera.2005.06.007.
Background: Previous evidence suggests that hydroxymethylglutaryl coenzyme A-reductase inhibitors (statins) might potentiate the effect of oral anticoagulants, but a MEDLINE search (key terms: stains, rosuvastatin, anticoagulants, Acenocoumarol, and interaction; years: 1980-2005) revealed no reports of an interaction between rosuvastatin and Acenocoumarol. Objective: The aim of this article was to describe a case of possible interaction between rosuvastatin and Acenocoumarol. Methods: We report the case of a 36-year-old male patient receiving long-term oral treatment with Acenocoumarol, a synthetic coumarin anticoagulant, who experienced an increase in international normalized ratio (INR) and a hematoma in the left leg approximately 45 days after the initiation of treatment with rosuvastatin. Results: After discontinuation of both drugs, an unexpectedly rapid decrease in INR was observed. Conclusions: Based on the results of this case, a possible pharmacologic interaction between rosuvastatin and Acenocoumarol should be considered. Rosuvastatin might enhance the anticoagulant effect of Acenocoumarol, and a rebound effect in cases of simultaneous discontinuation of both drugs might occur. Rosuvastatin should be administered with extreme caution in patients receiving long-term Acenocoumarol therapy.
[Switching from Acenocoumarol to phenprocoumon: step in personalised anticoagulation?]
Ned Tijdschr Geneeskd 2021 Sep 9;165:D5533.PMID:34523845doi
Acenocoumarol and phenprocoumon are vitamin K antagonists (VKA) with average half-lives of 11 hours and 160 hours, respectively. They are used to treat and prevent thrombosis in mechanical cardiac valve replacement, atrial fibrillation and venous thromboembolism. There are historical regional differences in preferred VKA in the Netherlands. Safe and effective treatment requires the international normalized ratios (INRs) to be in the therapeutic range, and stable. Theoretically, the longer-acting phenprocoumon would yield a higher time in therapeutic range (TTR) and lower INR variability. In practice, switching from Acenocoumarol to phenprocoumon eventually improves INR variability and in some patients TTR as well. However, during the preceding transition period, INRs are more often volatile and supratherapeutic. Furthermore, switching to an alternative VKA could weaken integrated care, as other healthcare providers are less experienced with it. Healthcare providers must coordinate an intended switch with the anticoagulation clinic.
Probable acenocoumarol-amoxycillin interaction
Acta Haematol 1993;90(4):195-7.PMID:8140860DOI:10.1159/000204457.
We present the case of a woman undergoing treatment with Acenocoumarol for deep vein thrombosis, who maintained an international normalized ratio (INR) of between 2.5 and 4 for 2 months. Seven days after the introduction of amoxycillin (500 mg/8 h) for a probable respiratory infection, the patient developed spontaneous bruising, with an INR of 7.1. Treatment with amoxycillin was discontinued, and 3 weeks later the INR had returned to previous values. In this case, the increase in the INR value with associated bruising after the addition of amoxycillin suggests a drug interaction between Acenocoumarol and amoxycillin, other possible causes having been eliminated.