Heparin sodium
(Synonyms: 肝素钠) 目录号 : GC10398
肝素钠作为抗凝剂，属于一类葡聚糖，可与多种蛋白质相互作用，产生多种生物活性。
Cas No.:9041-08-1
Sample solution is provided at 25 µL, 10mM.
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| Cell experiment [1]: | |
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Cell lines |
Mouse spermatozoa |
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Preparation Method |
Mouse spermatozoa were incubated with various concentrations (0.001-100 μM) of steroids (estrogen and progesterone) and heparin for 15 or 30 min, and then capacitation and AR were assessed using chlortetracycline. |
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Reaction Conditions |
0.001-100 μM; 15 or 30 min |
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Applications |
Steroids (estrogen and progesterone) and heparin studied effectively alter capacitation and/or AR in mouse spermatozoa with different manner. |
| Animal experiment [2]: | |
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Animal models |
Four- to six-week-old Athymic BALB/c-nu/nu female nude mice (14-18 g) |
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Preparation Method |
According to body weight and tumor size, the animals were divided into four experimental groups of five mice each: groups A, B, C, and D, respectively, received through the tail vein injections of 100 µL of saline as control (Group A, n=5), heparin (10 mg/kg, Group B, n=5), DOC-heparin VI (5 mg/kg, Group C, n=5), and DOC-heparin VI (10 mg/kg, Group D, n=5). Each drug was administered twice a week for four weeks after tumor inoculation. |
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Dosage form |
10 mg/kg; i.v. |
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Applications |
Larger antitumor effects of the DOC-heparin VI (8.5 mol of DOC coupled with 1.0 mol heparin) were achieved in animal studies, compared to heparin alone. |
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References: [1]. [1]Park YJ, et al. Xenoestrogenic chemicals effectively alter sperm functional behavior in mice. Reprod Toxicol. 2011 Dec;32(4):418-24. [2]. Cho KJ, et al. Preparation of sodium deoxycholate (DOC) conjugated heparin derivatives for inhibition of angiogenesis and cancer cell growth. Bioconjug Chem. 2008 Jul;19(7):1346-51. |
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Heparin sodium, as as anti-coagulants, belongs to a class of glucans, which can interact with a variety of proteins to produce a variety of biological activities.[1][2] Heparin sodium is routinely use for preventing the deep venous thrombosis in medical and surgical patients[5].
In vitro experiment it demonstrated that SARS-CoV-2 spike protein binds with a much higher affinity to heparin with K D of 55 nM compared to the RBD with K D of 1 μM alone. And heparin has no effect on angiotensin-converting enzyme 2 binding or proteolytic processing of the spike.[6] Moreover, heparin can inhibit the proteolytic activity of Mpro with an inhibition constant Ki of 6.9 nM and a half maximal inhibitory concentrations (IC50) of 7.8 ± 2.6 nM. [7].
In vivo clinical study it shown that treatment with continuous heparin sodium 12 500 U throughout 24 hours with intravenous pump for 5 days in heparin sodium group patients, and with low molecular weight heparin sodium (LMWHS) patients were given LMWHS 2 500 U subcutaneously, twice a day for 5 days, incidence of bleeding during treatment in LMWHS group was remarkably lower than that in heparin sodium group. Moreover, the platelet count in both LMWHS group and heparin sodium group was markedly increased compared with that before treatment; activated partial thromboplastin time also in heparin sodium group was significantly prolonged compared with that before treatment.[3] In the clinical test, there is no obvious difference in the duration of catheter patency or incidence of phlebitis was observed between the adult patients received 1 mL of a heparin sodium 100 units/mL flush solution and adult patients received a 0.9% sodium chloride flush solution by intermittent intravenous devices were randomly assigned.[4] In the clinical trail, treatment with low-dose heparin, patients with diabetes mellitus or chronic renal insufficiency are especially predisposed to hyperkalemia.[5].
References:
[1]Capila I, et al. Heparin-protein interactions. Angew Chem Int Ed Engl. 2002 Feb 1;41(3):391-412.
[2]Hashii N, et al. Heparin identification test and purity test for OSCS in heparin sodium and heparin calcium by weak anion-exchange high-performance liquid chromatography. Biologicals. 2010 Sep;38(5):539-43.
[3]Li Y, et al. [Comparison of the effect of low molecular weight heparin sodium and that of heparin sodium on pre-disseminated intravascular coagulation stage in patients suffering from exertional heat stroke]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Aug;27(8):649-52. Chinese.
[4]Hamilton RA, et al. Heparin sodium versus 0.9% sodium chloride injection for maintaining patency of indwelling intermittent infusion devices. Clin Pharm. 1988 Jun;7(6):439-43.
[5]Edes TE, et al. Heparin-induced hyperkalemia. Arch Intern Med. 1985 Jun;145(6):1070-2.
[6]Liu L, et al. Heparan Sulfate Proteoglycans as Attachment Factor for SARS-CoV-2. ACS Cent Sci. 2021 Jun 23;7(6):1009-1018.
[7]Li J, et al. Heparin interacts with the main protease of SARS-CoV-2 and inhibits its activity. Spectrochim Acta A Mol Biomol Spectrosc. 2022 Feb 15;267(Pt 2):120595.?
肝素钠作为抗凝剂，属于一类葡聚糖，可与多种蛋白质相互作用，产生多种生物活性。[1][2] 肝素钠常规用于预防内科和外科患者的深静脉血栓形成[5]。
体外实验表明，SARS-CoV-2 刺突蛋白与肝素的结合亲和力更高，K D 为 55 nM，而 RBD 单独使用时的 K D 为 1 μM。而肝素对血管紧张素转换酶2的结合或蛋白水解过程无影响。[6]此外，肝素可抑制Mpro的蛋白水解活性，抑制常数Ki为6.9 nM半。最大抑制浓度 (IC50) 为 7.8 ± 2.6 nM。 [7].
体内临床研究显示，肝素钠组患者24小时内连续12500U肝素钠静脉泵治疗5天，低分子肝素钠（LMWHS）患者给予LMWHS 2500U皮下给药，每天两次，连续5天，LMWHS组治疗期间的出血发生率明显低于肝素钠组。此外，LMWHS组和肝素钠组的血小板计数均较治疗前明显升高；肝素钠组活化部分凝血活酶时间也较治疗前显着延长。[3] 临床试验中，导管通畅时间及静脉炎发生率无明显差异在接受 1 mL 肝素钠 100 单位/mL 冲洗液的成年患者和通过间歇静脉装置接受 0.9% 氯化钠冲洗液的成年患者之间随机分配。[4] 在临床试验中、低剂量肝素治疗、糖尿病或慢性肾功能不全患者尤其容易发生高钾血症。[5]。
| Cas No. | 9041-08-1 | SDF | |
| 别名 | 肝素钠 | ||
| 化学名 | sodium (4S,6R)-6-(((2R,4R)-4,6-dihydroxy-5-(sulfonatoamino)-2-((sulfonatooxy)methyl)tetrahydro-2H-pyran-3-yl)oxy)-3,4-dihydroxy-5-(sulfonatooxy)tetrahydro-2H-pyran-2-carboxylate | ||
| Canonical SMILES | O[C@@H]1C(OS([O-])(=O)=O)[C@H](OC2[C@@H](COS([O-])(=O)=O)OC(O)C(NS([O-])(=O)=O)[C@H]2O)OC(C([O-])=O)C1O.[Na+].[Na+].[Na+].[Na+] | ||
| 分子式 | (C12H16NS2Na3)20 | 分子量 | 6000-20000 |
| 溶解度 | ≥ 12.75mg/mL in Water | 储存条件 | Store at 2-8°C , sealed storage, 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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| 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 | 0.1667 mL | 0.8333 mL | 1.6667 mL |
| 5 mM | 0.0333 mL | 0.1667 mL | 0.3333 mL |
| 10 mM | 0.0167 mL | 0.0833 mL | 0.1667 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。
Fabrication and characterisation of self-applicating heparin sodium microneedle patches
J Drug Target2021 Jan;29(1):60-68.PMID: 32649227DOI: 10.1080/1061186X.2020.1795180
The aim of this study was to develop heparin sodium loaded microneedle patches using different compositions of polyvinyl alcohol polymer and sorbitol. A vacuum micromolding technique was used to fabricate microneedle patches while heparin sodium was loaded into needle tips. Physical features of patches were evaluated by measuring thickness, width, folding endurance and swelling percentage. Patches were also characterised by optical microscopy and scanning electron microscopy to determine the microneedle length and surface morphologies. A preliminary assessment of the microneedle performance was studied by examining the in-vitro insertion to the parafilm and recording the in-vitro drug release profile. In-vivo activity of patches was confirmed by measuring activated partial thromboplastin time and histological examination of the micropierced skin tissues. Prepared patches were clear, smooth; uniform in appearance; with sharp pointed microprojections and remained intact after 1000 folding. The microneedles were stiffer in nature, as they reproduce microcavities in the parafilm membrane following hand pushing without any structural loss. Insertion study results showed successful insertion of microneedles into the parafilm. Disrupted stratum corneum evident from histological examination confirmed successful insertion of the microneedle without affecting the vasculature. In-vitro release study confirmed ∼92% release of the loaded drug within 120 min. A significant prolongation of activated partial thromboplastin time (4 folds as compared to negative control) was recorded following the application of heparin sodium loaded microneedle patch onto rabbit skin. In conclusion microneedles are a valuable drug delivery system, benefiting the patients with minimal skin invasion and also allowing self-administration of heparin sodium in a sustained release manner for the management of chronic ailments.
Inhaled Heparin: Therapeutic Efficacy and Recent Formulations
J Aerosol Med Pulm Drug Deliv2017 Jun;30(3):143-156.PMID: 28418758DOI: 10.1089/jamp.2015.1273
Heparin is well known for its anticoagulant and anti-inflammatory properties. Inhaled heparin regimens are increasingly being used to manage lung disease. It has been used to treat cystic fibrosis, thromboembolism, and pulmonary fibrosis, as well as bronchial asthma and asthma-induced airway hypersensitivity. Several preclinical studies attained some useful effects of heparin-administered, parenterally and through inhalation, treatment of lung disease. Besides, recent clinical trials suggest that inhaled heparin for lung diseases is beneficial and safe, but such data remain to be limited. In 2005, the orphan designation was granted by the European Commission for heparin sodium (inhalation use) for the treatment of cystic fibrosis. The positive results of heparin in the pulmonary route necessitate a focus on the preparation and evaluation of heparin in advanced drug delivery systems, namely nano/microparticles and liposomes. Through this pulmonary delivery, heparin is protected from enzymatic degradation within the airway. Heparin is thus passively targeted into the lungs, and long-lasting localized treatment is achieved. On the other hand, these systems have encountered several problems as follows: (1) polymers, such as poly-L-lactide-glycolic acid, poly (lactic acid), and chitosan, used to prepare heparin-loaded microparticle/nanoparticle (MP/NP) systems have not been granted approval for lung application by the FDA and (2) liposomal and NP formulation stability is the main problem of formulation design. We propose that additional in vitro and in vivo research is necessary to assess the clinical applicability of this treatment strategy. The present article discusses heparin treatments for lung diseases and the use of heparin and/or heparin-loaded drugs in advanced delivery systems through the pulmonary route.
Efficacy of vitamin E combined with heparin sodium cream in treatment of scleredema neonatorum
Panminerva Med2021 Jun;63(2):240-241.PMID: 31355597DOI: 10.23736/S0031-0808.19.03687-5
Objective: To investigate the clinical effect of low molecular weight heparin sodium combined with antivenin in the treatment of severe and critical bite by Trimeresurus stejnegeri.
Methods: The clinical data of 48 patients with severe or critical bite by Trimeresurus stejnegeri admitted to emergency department of Southeast Hospital Affiliated to Xiamen University from March 2017 to May 2019 were retrospectively analyzed. On the basis of early treatment of antivenom serum, internal administration and external application of Jidesheng snake tablet, and wound incision and detoxification, the patients were divided into heparin treatment group and non-heparin treatment group according to whether the low molecular heparin sodium was used or not. The patients in the two groups were compared in terms of gender, age, clinical classification, swelling degree of injured limbs, change of coagulation function index, bleeding of skin, mucous membrane or digestive tract, blood transfusion, local symptoms of bite, length of hospital stay and prognosis.
Results: There was no significant difference in terms of gender, age, clinical classification or swelling degree of injured limbs between the two groups. On the 3rd day of treatment, the platelet count (PLT) in the heparin treatment group was significantly higher than that in the non-heparin treatment group [×109/L: 210.0 (160.0, 252.0) vs. 136.0 (104.0, 198.5), P < 0.05]. However, there was no significant difference in the four coagulation test results between the two groups. On the 6th day of treatment, the plasma thrombin time (TT) in the heparin treatment group was significantly shorter than that on the 3rd day of treatment [s: 30.3 (20.4, 37.0) vs. 34.7 (24.0, 73.4), P < 0.05], and the fibrinogen (FIB) in the heparin treatment group was significantly higher than that in the non-heparin treatment group [g/L: 0.60 (0.31, 1.07) vs. 0.20 (0.14, 0.60), P < 0.01]. The incidence of bleeding in the heparin treatment group was significantly lower than that in the non-heparin treatment group [21.7% (5/23) vs. 64.0% (16/25), P < 0.01]; 11 patients in the heparin treatment group and 18 patients in the non-heparin treatment group received blood transfusion and prothrombin complex supplement respectively. There was no significant difference in the length of hospital stay between the heparin group and non-heparin treatment group (days: 6.91±1.92 vs. 7.48±2.27, P > 0.05). The patients in both groups were followed up for 1 week to 1 month after treatment, and no death or local necrosis of skin and soft tissue was found.
Conclusions: For the patients with severe and critical bite by Trimeresurus stejnegeri, on the basis of injection of antivenom serum, internal administration and external application of Jidesheng snake tablet, and wound incision and detoxification, early application of low molecular weight heparin sodium anticoagulation and other comprehensive treatment is helpful to improve limb swelling and inflammation, reduce blood transfusion, promote the recovery of coagulation function, and shorten the length of hospitalization.
[A real-world study of low molecular weight heparin sodium in the treatment of severe and critical bite by Trimeresurus stejnegeri]
Zhonghua Wei Zhong Bing Ji Jiu Yi Xue2020 May;32(5):601-604.PMID: 32576355DOI: 10.3760/cma.j.cn121430-20200204-00166
Objective: To investigate the clinical effect of low molecular weight heparin sodium combined with antivenin in the treatment of severe and critical bite by Trimeresurus stejnegeri.
Methods: The clinical data of 48 patients with severe or critical bite by Trimeresurus stejnegeri admitted to emergency department of Southeast Hospital Affiliated to Xiamen University from March 2017 to May 2019 were retrospectively analyzed. On the basis of early treatment of antivenom serum, internal administration and external application of Jidesheng snake tablet, and wound incision and detoxification, the patients were divided into heparin treatment group and non-heparin treatment group according to whether the low molecular heparin sodium was used or not. The patients in the two groups were compared in terms of gender, age, clinical classification, swelling degree of injured limbs, change of coagulation function index, bleeding of skin, mucous membrane or digestive tract, blood transfusion, local symptoms of bite, length of hospital stay and prognosis.
Results: There was no significant difference in terms of gender, age, clinical classification or swelling degree of injured limbs between the two groups. On the 3rd day of treatment, the platelet count (PLT) in the heparin treatment group was significantly higher than that in the non-heparin treatment group [×109/L: 210.0 (160.0, 252.0) vs. 136.0 (104.0, 198.5), P < 0.05]. However, there was no significant difference in the four coagulation test results between the two groups. On the 6th day of treatment, the plasma thrombin time (TT) in the heparin treatment group was significantly shorter than that on the 3rd day of treatment [s: 30.3 (20.4, 37.0) vs. 34.7 (24.0, 73.4), P < 0.05], and the fibrinogen (FIB) in the heparin treatment group was significantly higher than that in the non-heparin treatment group [g/L: 0.60 (0.31, 1.07) vs. 0.20 (0.14, 0.60), P < 0.01]. The incidence of bleeding in the heparin treatment group was significantly lower than that in the non-heparin treatment group [21.7% (5/23) vs. 64.0% (16/25), P < 0.01]; 11 patients in the heparin treatment group and 18 patients in the non-heparin treatment group received blood transfusion and prothrombin complex supplement respectively. There was no significant difference in the length of hospital stay between the heparin group and non-heparin treatment group (days: 6.91±1.92 vs. 7.48±2.27, P > 0.05). The patients in both groups were followed up for 1 week to 1 month after treatment, and no death or local necrosis of skin and soft tissue was found.
Conclusions: For the patients with severe and critical bite by Trimeresurus stejnegeri, on the basis of injection of antivenom serum, internal administration and external application of Jidesheng snake tablet, and wound incision and detoxification, early application of low molecular weight heparin sodium anticoagulation and other comprehensive treatment is helpful to improve limb swelling and inflammation, reduce blood transfusion, promote the recovery of coagulation function, and shorten the length of hospitalization.