Enoxaparin
(Synonyms: PK 10169; Enoxaparin sodium; Lovenox) 目录号 : GC68034Enoxaparin (PK 10169) 是一种低分子肝素 (LMWH) 衍生物。Enoxaparin 通过抗凝血酶 III 发挥其抗凝血 (anticoagulant) 活性，抗凝血酶 III 是一种内源性 Xa 因子和凝血酶 IIa (thrombin IIa) 的抑制剂。Enoxaparin 可通过抗氧化 (antioxidant) 和抗炎 (anti-inflammatory) 作用保护大鼠海马区免受 TBI 损伤。Enoxaparin 可用于深静脉血栓形成 (DVT)、肺栓塞、外伤性脑损伤 (TBI) 和 COVID-19 的研究。
Cas No.:679809-58-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of Factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19[1][2][3].
Enoxaparin (0-70 µg/mL, 90 min) enhances AAT (alpha-1-antitrypsin) inhibition of both TMPRSS2 (Transmembrane Protease 2) activity and infection of hAEc (human airway epithelial cells) with HCoV-229E[1].
Cell Viability Assay[1]
| Cell Line: | HEK293T TMPRSS2 cells, hAEc |
| Concentration: | 0, 8.8, 35, 70 µg/mL |
| Incubation Time: | 90 min |
| Result: | Significantly inhibited TMPRSS2 activity at the 90 min incubation period at 35 and 70 µg/mL, enhanced AAT inhibition of TMPRSS2 activity, and augmented AAT inhibition of HCoV-229E infection of hAEc. |
Enoxaparin (1 mg/kg; SC; once every 6 h for 8 times) reduces oxidative damage, inflammation and astrocytosis following TBI (traumatic brain injury) in the rat[2].
| Animal Model: | Adult male Wistar rats (350-450 g, TBI-treated)[2] |
| Dosage: | 0 mg/kg, 1 mg/kg |
| Administration: | SC, once every 6 h, starting at 1 h, and finishing at 43 h after the TBI induction. |
| Result: | Significantly decreased the hippocampal TBARS and oxidized protein levels, COX-2 overexpression and reactive gliosis, but it did not influence the SOD and GSH-Px activities, pro-IL-1β and active caspase-3 overexpressions as well as neurodegeneration following TBI. Reduce oxidative damage, inflammation and astrocytosis following TBI in the rat. |
[1]. Bai X, et al. Enoxaparin augments alpha-1-antitrypsin inhibition of TMPRSS2, a promising drug combination against COVID-19. Sci Rep. 2022 Mar 25;12(1):5207.
[2]. ?upan ?, et al. Effects of enoxaparin in the rat hippocampus following traumatic brain injury. Prog Neuropsychopharmacol Biol Psychiatry. 2011 Dec 1;35(8):1846-56.
[3]. Lee S, Gibson CM. Enoxaparin in acute coronary syndromes. Expert Rev Cardiovasc Ther. 2007 May;5(3):387-99.
| Cas No. | 679809-58-6 | SDF | Download SDF |
| 别名 | PK 10169; Enoxaparin sodium; Lovenox | ||
| 分子式 | 分子量 | ||
| 溶解度 | H2O : ≥ 100 mg/mL | 储存条件 | 4°C, protect from light |
| 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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每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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Pharmacodynamic and pharmacokinetic properties of Enoxaparin : implications for clinical practice
Clin Pharmacokinet 2003;42(12):1043-57.PMID:12959635DOI:10.2165/00003088-200342120-00003.
Enoxaparin is a low-molecular-weight heparin (LMWH) that differs substantially from unfractionated heparin (UFH) in its pharmacodynamic and pharmacokinetic properties. Some of the pharmacodynamic features of Enoxaparin that distinguish it from UFH are a higher ratio of anti-Xa to anti-IIa activity, more consistent release of tissue factor pathway inhibitor, weaker interactions with platelets and less inhibition of bone formation. Enoxaparin has a higher and more consistent bioavailability after subcutaneous administration than UFH, a longer plasma half-life and is less strongly bound to plasma proteins. These properties mean that Enoxaparin provides a more reliable anticoagulant effect without the need for laboratory monitoring, and also offers the convenience of once-daily administration. Clinical studies have confirmed that these pharmacological advantages translate into improved outcomes. There are important pharmacokinetic and pharmacodynamic differences between Enoxaparin, other LMWHs and UFH, and therefore these molecules cannot be regarded as interchangeable.
Safety and Efficacy of Enoxaparin in Pregnancy: A Systematic Review and Meta-Analysis
Adv Ther 2020 Jan;37(1):27-40.PMID:31673991DOI:10.1007/s12325-019-01124-z.
Introduction: International guidelines support the use of low molecular weight heparins for the treatment of thromboembolism and thromboprophylaxis during pregnancy. However, evidence of the benefit and harm associated with specific low molecular weight heparins such as Enoxaparin is dated. No current systematic review and meta-analysis describing the safety and efficacy of Enoxaparin for thromboembolism and thromboprophylaxis during pregnancy exists. Methods: PubMed, Embase, and Cochrane databases were searched on August 17, 2018 for clinical trials or observational studies in pregnant women receiving Enoxaparin; patients with a prosthetic heart valve were excluded. Risk ratios (RR) with 95% confidence intervals (CI) were calculated using a random effects model, and heterogeneity was measured using the I2 statistic. Results: Of the 485 records identified in the search, 24 studies published clinical trials, and observational studies were found dating back to 2000. Only one observational cohort and one randomized control trial focused on the use of Enoxaparin for thromboprophylaxis and therefore efficacy was not assessed; the other studies included women with recurrent pregnancy loss (15 studies), history of placental vascular complications (five studies), and recurrent in vitro fertilization failure (two studies) and were therefore analyzed in terms of safety only. Bleeding events were non-significantly more often reported for Enoxaparin compared to untreated controls (RR 1.35 [0.88-2.07]) but less often reported for Enoxaparin versus aspirin (RR 0.93 [0.62-1.39]); thromboembolic events, thrombocytopenia, and teratogenicity were rarely reported events; in patients with a history of recurrent pregnancy loss, encouragingly the rates of pregnancy loss were significantly lower for Enoxaparin compared to untreated controls (RR 0.58 [0.34-0.96]) and Enoxaparin + aspirin versus aspirin alone (RR 0.42 [0.32-0.56]) as well as observably lower for Enoxaparin versus aspirin alone (RR 0.39 [0.15-1.01]), though significant heterogeneity was observed (I2 > 60). Conclusion: Literature on the efficacy and safety of Enoxaparin for thromboembolism and thromboprophylaxis remains scanty, and therefore efficacy was not assessed; in terms of safety, when including other indications for Enoxaparin in pregnancy, we found that Enoxaparin was associated with significantly lower complications than aspirin. Given differences in study design and study heterogeneity, pregnancy loss results should be interpreted with caution. Moreover, reports of thromboembolic events, thrombocytopenia, and congenital malformations were rare. Funding: Sanofi.
Enoxaparin in acute coronary syndromes
Expert Rev Cardiovasc Ther 2007 May;5(3):387-99.PMID:17489664DOI:10.1586/14779072.5.3.387.
Enoxaparin is a low-molecular-weight heparin (LMWH) derivative that exerts its anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Unlike its unfractionated heparin (UFH) counterparts, Enoxaparin has a greater bioavailability, lower incidence of heparin-induced thrombocytopenia and more stable and predictable anticoagulation, allowing fixed dosing without the need for monitoring. These advantages make it an attractive anticoagulant to be used in acute coronary syndrome management. Indeed, several clinical trials and meta-analyses have consistently demonstrated the efficacy of Enoxaparin in reducing cardiovascular events and mortality in this population. Although initial clinical trials with Enoxaparin during the early conservative approach suggested superior efficacy without differences in safety compared with UFH, emerging data in the current era of early revascularization approach indicate that superior effects of Enoxaparin over heparin in reducing clinical events should be balanced against an increase in major hemorrhagic complications. Enoxaparin is a rational alternative to UFH in patients presenting with either unstable angina/non-ST-elevation myocardial infarction or ST-elevation myocardial infarction, with a clinically modest increase in bleeding complications.
Enoxaparin for neonatal thrombosis: a call for a higher dose for neonates
Thromb Res 2008;122(6):826-30.PMID:18207492DOI:10.1016/j.thromres.2007.11.009.
Introduction: Enoxaparin is the current anticoagulant of choice for neonatal thrombosis. Present neonatal treatment guidelines of 1.5 mg/kg every 12 hours (q12 h) are extrapolated primarily from an earlier study with 9 infants less than 2 months of age. More recent studies indicate an increased dose requirement for neonates. Materials and methods: Relevant data from articles and abstracts were identified by searching MEDLINE and pediatric and hematology conference proceedings. Results: Publications between 1996 and 2007 included 8 papers, 4 abstracts and 1 review article with primary research documenting Enoxaparin use in 240 neonates. The mean maintenance dose of Enoxaparin ranged from 1.48 to 2.27 mg/kg q12 h for all infants, but was higher for preterm neonates at 1.9-2.27 mg/kg q12 h. The efficacy of Enoxaparin, causing either complete or partial resolution was between 59 and 100%. Minor side effects were common and adverse events (major bleeding) occurred in 12 patients (0-19%). Conclusions: Increased experience with Enoxaparin use in neonates in the past decade has indicated higher doses to achieve accepted target anti-factor Xa values. The long-term use of indwelling catheters (Insuflon catheter) for Enoxaparin administration may need to be reevaluated in ELBW infants. Suggested starting doses of Enoxaparin are 1.7 mg/kg q12 h for term neonates and 2.0 mg/kg q12 h for preterm neonates if there is no considerable bleeding risk. However, further prospective studies are needed to validate an increased initial dose of Enoxaparin.
Enoxaparin: an update of its clinical use in the management of acute coronary syndromes
Drugs 2002;62(9):1407-30.PMID:12076195DOI:10.2165/00003495-200262090-00017.
Enoxaparin (Enoxaparin sodium) is a low molecular weight heparin (LMWH) indicated for use in the treatment of ischaemic complications of unstable angina and non-Q wave myocardial infarction (MI). Unfractionated heparin (UFH) has for many years represented the standard in anticoagulant therapy for patients with acute coronary syndromes; however, recent studies suggest that Enoxaparin is also a viable option for anticoagulant therapy in these patients. The ESSENCE (Efficacy and Safety of Subcutaneous Enoxaparin in Non-Q wave Coronary Events) and the TIMI 11B (Thrombolysis in Myocardial Infarction) studies reported that twice daily Enoxaparin was significantly more effective than a continuous infusion of UFH in reducing the composite triple endpoint of death, MI, or recurrent angina or urgent revascularisation. Follow-up of both patient populations showed continued benefit associated with Enoxaparin. Enoxaparin has been compared with tinzaparin in the treatment of unstable coronary artery disease using a nonblind study design. There was no difference between treatment groups in the therapeutic endpoints. Three nonblind studies have also compared the effects of Enoxaparin and UFH in patients receiving thrombolytic therapy following acute MI. The HART II (Heparin and Aspirin Reperfusion Therapy), the ASSENT 3 (Assessment of the Safety and Efficacy of a New Thrombolytic Regimen) and the ENTIRE-TIMI 23 (Enoxaparin and Tenecteplase with or without glycoprotein IIb/IIIa Inhibitor as Reperfusion strategy in ST Elevation MI - Thrombolysis in Myocardial Infarction) studies have revealed that Enoxaparin in combination with alteplase or tenecteplase is at least equivalent (HART II and ENTIRE-TIMI 23), and possibly superior (ASSENT 3) to UFH. Enoxaparin is administered as a twice-daily subcutaneous injection. In contrast, UFH is administered as an intravenous infusion which requires routine monitoring of the activated partial thromboplastin time to ensure adequate levels of anticoagulation are maintained. During the acute phase of the the ESSENCE and TIMI 11B studies, the incidence of major bleeding was similar in patients receiving Enoxaparin to that in patients receiving UFH. In contrast, the rates of minor bleeding were higher in patients receiving Enoxaparin than in those receiving UFH throughout these studies. Conclusions: Data from the ESSENCE, TIMI 11B and ASSENT 3 studies have prompted calls for those LMWHs which have been shown to be superior to UFH, to be considered as first choice treatment for anticoagulation in unstable coronary syndromes. To date, these suggestions are not reflected in current guidelines which consider UFH and LMWHs equally. Irrespective, the clinical data reported in this review support the use of Enoxaparin in the treatment of acute coronary syndromes. These data suggest that Enoxaparin shows certain clinical and practical advantages over standard treatment with UFH and represents an important development in the treatment of acute coronary syndromes.