Protamine sulfate
(Synonyms: 原儿茶醛) 目录号 : GC62048
Protamine sulfate 是一个阳性离子肽，具有抗肝素活性，可以中和肝素的抗凝血作用，增强脂质介导的基因转移。
Cas No.:9009-65-8
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
Protamine sulfate, polycationic peptide and a antiheparin agent, could neutralize the anticoagulant action of heparin and enhances lipid-mediated gene transfer[1][2][3].
Protamine sulfate has an inhibitory effect on thrombin in the conversion of fibrinogen to fibrin, and that this inhibition is concentration dependent, partial, and reversible[3].Protamine sulfate is a 5-kDa cationic polypeptide derived from salmon sperm that can bind negatively charged unfractionated heparin (UFH). Protamine sulfate down-regulates thrombin generation by inhibiting factor V activation[4].
[1]. Ahmed Kouta, et al. Protamine Sulfate Neutralization Profile of Various Dosages of Bovine, Ovine and Porcine UFHs and Their Depolymerized Derivatives in Non-Human Primates. Clin Appl Thromb Hemost. Jan-Dec 2021;27:10760296211005544.
[2]. F L Sorgi, et al. Protamine sulfate enhances lipid-mediated gene transfer. Gene Ther. 1997 Sep;4(9):961-8.
[3]. R J Cobel-Geard, et al. Interaction of protamine sulfate with thrombin. Am J Hematol. 1983 May;14(3):227-33.
[4]. Fionnuala Ni Ainle, et al. Protamine sulfate down-regulates thrombin generation by inhibiting factor V activation. Blood. 2009 Aug 20;114(8):1658-65.
| Cas No. | 9009-65-8 | SDF | |
| 别名 | 原儿茶醛 | ||
| 分子式 | 分子量 | ||
| 溶解度 | H2O : ≥ 33.33 mg/mL | 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。 | ||
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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。
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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。
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Allergy to Protamine sulfate
Heart Lung 1999 Nov-Dec;28(6):418-28.PMID:10580216DOI:10.1016/s0147-9563(99)70031-2.
Adverse responses to Protamine sulfate have been identified for many years. The antigen-antibody response to Protamine sulfate results in a type I anaphylactic reaction. Manifestations of allergic reactions include hypotension, bronchospasm, and skin and mucous membrane reactions. The severity of the adverse responses may vary from mild to causing death. Several potential risk factors for adverse reactions to protamine have been identified, including insulin-dependent diabetes mellitus, vasectomy, allergy to fish, prior exposure to Protamine sulfate, and the rate of infusion. A case study is presented, and strategies for improving patient outcomes are discussed.
Protamine sulfate Is a Potent Inhibitor of Human Papillomavirus Infection In Vitro and In Vivo
Antimicrob Agents Chemother 2022 Jan 18;66(1):e0151321.PMID:34723633DOI:10.1128/AAC.01513-21.
Human papillomavirus (HPV) infections are transmitted through sexual or other close contact and are etiologically associated with epithelial warts, papillomas, and intraepithelial lesions that may progress to cancer. Indeed, 4.8% of the global cancer burden is linked to HPV infection. Highly effective vaccines protect against two to nine of the most medically important HPV genotypes, yet vaccine uptake is inadequate and/or cost prohibitive in many settings. With HPV-related cancer incidence expected to rise over the coming decades, there is a need for effective HPV microbicides. Herein, we demonstrate the strong inhibitory activity of the heparin-neutralizing drug Protamine sulfate (PS) against HPV infection. Pretreatment of cells with PS greatly reduced infection, regardless of HPV genotype or virus source. Vaginal application of PS prevented infection of the murine genital tract by HPV pseudovirions. Time-of-addition assays where PS was added to cells before infection, during infection, or after viral attachment demonstrated strong inhibitory activities on early infection steps. No effect on virus infection was found for cell lines deficient in heparan sulfate expression, suggesting that PS binds to heparan sulfate on the cell surface. Consistent with this, prophylactic PS exposure prevented viral attachment, including under low-pH conditions akin to the human vaginal tract. Our findings suggest PS acts dually to prevent HPV infection: prophylactic treatment prevents HPV attachment to host cells, and postattachment administration alters viral entry. Clinical trials are warranted to determine whether protamine-based products are effective as topical microbicides against genital HPVs.
Protamine sulfate use during tibial bypass does not appear to increase thrombotic events or affect short-term graft patency
Vascular 2020 Dec;28(6):708-714.PMID:32393108DOI:10.1177/1708538120924149.
Objectives: While the use of Protamine sulfate as a heparin reversal agent has been extensively reviewed in patients undergoing carotid endarterectomy and coronary artery bypass grafting, there is a lack of literature on protamine's effects on lower extremity bypasses. The purpose of this study was to determine the risk of Protamine sulfate dosing after tibial bypass on thrombotic or bleeding events, including early bypass failure. Methods: We performed a retrospective review of our institutional database for patients undergoing primary distal peripheral bypass from January 2009 through December 2015 (contralateral bypass was considered to be a new primary bypass). Primary endpoints include composite thrombotic events (myocardial infarction, stroke, amputation at 30 days and patency less than 30 days) and composite bleeding events (bleeding or transfusion). Results: A total of 152 tibial or peroneal bypasses in 136 patients with critical limb ischemia were identified. Of these, 78 (57.4%) patients received Protamine sulfate intraoperatively and 58 (42.6%) did not. There were no differences in composite thrombotic or hemorrhagic outcomes. Protamine use had no effect on the rates of perioperative MI (9.0% versus 3.5%, p = 0.20), stroke (1.3% versus 1.7%, p = 0.83), or perioperative mortality (5.1% versus 3.5%, p = 0.64). There was no significant difference in composite post-operative bleeding events (20.7% versus 14.1%, p = 0.31) or composite thrombotic events (17.2% versus 18.0%, p = 0.91). Patients who received protamine undergoing bypass with non-autogenous conduit had significantly higher-recorded median operative blood loss (250 mL versus 150 mL, p = 0.0097) and median procedure lengths (265 min versus 201 min, p = 0.0229). No difference in 30-day amputation-free survival was noted (91.0% versus 91.4%, p = 0.94). Follow-up Kaplan-Meier estimation did not demonstrate a difference in 30-day patency (91.7% versus 88.5%, p = 0.52). Conclusions: Heparin reversal with Protamine sulfate after tibial or peroneal bypass grafting is not associated with higher cardiovascular morbidity, bypass thrombosis, amputation, or mortality. Additionally, there was no statistically significant difference in post-operative bleeding or thrombosis complications for patients who did not receive protamine, although the findings are suggestive of a potential difference in a more adequately powered study. Our results suggest that Protamine sulfate is safe for intraoperative use without increased risk of thrombotic complications or early tibial bypass graft failure.
Serious anaphylactic reactions due to Protamine sulfate: a systematic literature review
Basic Clin Pharmacol Toxicol 2008 Aug;103(2):192-6.PMID:18816305DOI:10.1111/j.1742-7843.2008.00274.x.
Anaphylactic reactions caused by injection of Protamine sulfate during cardiac surgery are a well-known complication. A systematic literature review was therefore conducted to gather evidence of the knowledge concerning these side effects, and to see if any prospective randomized studies supported this. Studies investigating the effect of Protamine sulfate in human beings were extracted from MEDLINE, Embase and the Cochrane Library, retrieving 487 articles. Abstracts were evaluated by both authors, and referred articles not found in the primary search were furthermore extracted from reviews and case reports, resulting in a total of 272 relevant articles. Of these, 9 retrospective studies and 16 prospective studies were performed in an evidence-based manner. However, only 3 of the 16 prospective articles had an optimal design as far as inclusion criteria, randomization, and description of symptoms were concerned. Incidence of anaphylactic reactions in the prospective studies was 0.69% compared to 0.19% in the retrospective studies, but caution should be taken due to a pronounced heterogeneity of those studies. One study found heparinase I unsuitable as replacement for Protamine sulfate. Overall, our findings support the low incidence of anaphylactic reactions reported in previous studies, but of note only few prospective investigations was conducted on the subject. Our study also emphasizes the need for critical appraisal of many routine procedures: in all aspects of medical care, systematic literature review conducted in a well-structured, repeated manner should be given high priority.
Protamine sulfate during transcatheter aortic valve implantation (PS TAVI) - a single-center, single-blind, randomized placebo-controlled trial
Kardiol Pol 2021;79(9):995-1002.PMID:34292562DOI:10.33963/KP.a2021.0070.
Background: Bleeding complications after transcatheter aortic valve implantation (TAVI) negatively affect the post-procedural prognosis. Routine use of Protamine sulfate (PS) to reverse unfractionated heparin after TAVI was never assessed in a randomized controlled trial. Aims: The aim of this study was to assess the impact of PS on bleeding complications after TAVI. Methods: Between December 2016 and July 2020 311 patients qualified to TAVI in one academic center were screened. Patients that met the inclusion criteria were randomized to either PS or normal saline administration at the moment of optimal valve deployment. Baseline, procedural, and follow-up data for up to 30 days were collected and analyzed. The primary endpoint (PE) was a composite of life-threatening and major bleeding according to Valve Academic Research Consortium within 48 hours after the procedure. Results: Overall, 100 patients (48 males, median age 82 years) met the inclusion criteria and were included in the study. Forty-seven subjects (47%) were randomized to PS. The primary endpoint occurred in 29% of the study population. Despite numerically lower rates of PE in patients randomized to PS, a statistical significance was not reached (21% in the PS group and 36% in the placebo group; odds ratio [OR], 0.48; 95% confidence intervals [CI] 0.2-1.2; P = 0.11). There were no significant differences in secondary endpoints. Conclusions: Routine Protamine sulfate administration did not significantly decrease the rate of major and life-threatening bleeding complications after TAVI. Larger studies are required to assess the impact of routine PS use.