Pocapavir (SCH-48973)
(Synonyms: SCH-48973; V-073) 目录号 : GC32120
Pocapavir (SCH-48973) (SCH-48973) 是一种具有口服活性的衣壳抑制剂。
Cas No.:146949-21-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pocapavir is an investigational enterovirus (EV) capsid inhibitor.
Pocapavir acts as a capsid inhibitor, preventing virion uncoating upon entry into the cell. Treatment with Pocapavir is safe and significantly accelerates virus clearance[1]. Pocapavir, an investigational oral antiviral, has been used in a case of neonatal enterovirus sepsis. Pocapavir, also known as SCH 48973 and V-073, is a potent, selective anti-enteroviral agent only available as an emergency investigational drug. Pocapavir belongs to a picornavirus antiviral mechanistic class called capsid inhibitors that block virus uncoating and viral RNA release into cells, which in turn prevents virus replication[2].
[1]. Collett MS, et al. Antiviral Activity of Pocapavir in a Randomized, Blinded, Placebo-Controlled Human Oral Poliovirus Vaccine Challenge Model. J Infect Dis. 2017 Feb 1;215(3):335-343. [2]. Wittekind SG, et al. Neonatal Enterovirus Myocarditis With Severe Dystrophic Calcification: Novel Treatment WithPocapavir. J Investig Med High Impact Case Rep. 2017 Sep 14;5(3):2324709617729393.
| Cas No. | 146949-21-5 | SDF | |
| 别名 | SCH-48973; V-073 | ||
| Canonical SMILES | ClC1=C(OCC2=CC=C(COC3=CC=C(OC)C=C3Cl)C=C2)C(Cl)=CC=C1 | ||
| 分子式 | C21H17Cl3O3 | 分子量 | 423.72 |
| 溶解度 | DMSO : 100 mg/mL (236.00 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 2.36 mL | 11.8002 mL | 23.6005 mL |
| 5 mM | 0.472 mL | 2.36 mL | 4.7201 mL |
| 10 mM | 0.236 mL | 1.18 mL | 2.36 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。
Clinical characteristics of severe neonatal enterovirus infection: a systematic review
BMC Pediatr2021 Mar 15;21(1):127.PMID:33722228DOI:10.1186/s12887-021-02599-y.
Background: Enterovirus (EV) is a common cause of infection in neonates. Neonates are at high risk of enterovirus infection with serious clinical manifestations and high lethality. This review systematically summarized the clinical characteristics of neonates with severe enteroviral infection to provide evidence for the identification and treatment of severe neonatal EV infection. Methods: PubMed, Embase, and Web of Science were searched for original studies on neonates with severe EV infections from January 1, 2000, to November 27, 2020. Two reviewers independently screened the literature, extracted the data, and performed a descriptive analysis. Results: In total, 66 articles with 237 cases of severe neonatal enterovirus infection were included. All neonates developed severe complications. Among them, 46.0% neonates had hepatitis or coagulopathy, 37.1% had myocarditis, 11.0% had meningoencephalitis, and 5.9% had other complications such as hemophagocytic lymphohistiocytosis and pulmonary hemorrhage. The lethality rate of neonates with severe infection was 30.4%. The highest lethality rate was 38.6%, which was observed in neonates with myocarditis. In 70.5% neonates, the age at the onset of symptoms was less than 7 days. Coxsackievirus B infection was seen in 52.3% neonates. The most common symptoms included temperature abnormalities (127, 53.6%), rash (88, 37.1%), poor feeding (58, 24.5%), and respiratory symptoms (52, 21.9%). The main treatment included transfusion of empirical antibiotics (127, 53.6%), blood components (100, 42.2%), intravenous immunoglobulin (IVIG; 97, 40.9%), mechanical ventilation (51, 21.5%), and extracorporeal membrane oxygenation (ECMO; 43, 18.1%). Additionally, antiviral medications pleconaril (14, 5.9%) and Pocapavir (3, 1.3%) were administered. Conclusions: Lethality was high in neonates with severe enterovirus infection, especially in those complicated with myocarditis. The most common symptoms included temperature abnormalities, rash, and poor feeding. The chief supportive treatment consisted of transfusion of blood components, mechanical ventilation, and ECMO. Empirical antibiotics and IVIG were widely used. Antiviral medications included Pocapavir and pleconaril; however, more clinical evidence regarding their efficacy is needed.
Neonatal nonpolio enterovirus and parechovirus infections
Semin Perinatol2018 Apr;42(3):191-197.PMID:29526382DOI:10.1053/j.semperi.2018.02.007.
Nonpolio enteroviruses and parechoviruses are frequent causes of neonatal infection. Clinical manifestations of infection range from asymptomatic infection to mild infection without sequelae to septic shock with muiltiorgan failure. Neonates with clinically apparent infection typically have mothers and/or other contacts with recent symptoms consistent with a viral illness. Severe neonatal infection with nonpolio enterovirus or parechovirus cannot be differentiated clinically from serious bacterial infection. The preferred method for diagnosing neonatal nonpolio enterovirus or parechovirus infection is PCR as it is rapid, sensitive, specific, and commercially available for the detection of virus from various clinical specimens. Investigational agents such as the capsid inhibitors pleconaril and Pocapavir show promise for treatment of neonatal enterovirus infections, and other investigational agents are being developed. This review focuses on the epidemiology, diagnosis, and treatment of neonatal nonpolio enterovirus and parechovirus infections.
Update on nonpolio enterovirus and parechovirus infections in neonates and young infants
Curr Opin Pediatr2023 Mar 6.PMID:36876331DOI:10.1097/MOP.0000000000001236.
Purpose of review: To review the epidemiology, clinical manifestations, and treatment strategies of nonpolio enterovirus and parechovirus (PeV) infections, and identify research gaps. Recent findings: There is currently no approved antiviral agent for enterovirus or PeV infections, although Pocapavir may be provided on a compassionate basis. Elucidation of the structure and functional features of enterovirus and PeV may lead to novel therapeutic strategies, including vaccine development. Summary: Nonpolio human enterovirus and PeV are common childhood infections that are most severe among neonates and young infants. Although most infections are asymptomatic, severe disease resulting in substantial morbidity and mortality occurs worldwide and has been associated with local outbreaks. Long-term sequelae are not well understood but have been reported following neonatal infection of the central nervous system. The lack of antiviral treatment and effective vaccines highlight important knowledge gaps. Active surveillance ultimately may inform preventive strategies.
Coordinated Response to Imported Vaccine-Derived Poliovirus Infection, Barcelona, Spain, 2019-2020
Emerg Infect Dis2021 May;27(5):1513-1516.PMID:33900188DOI:10.3201/eid2705.204675.
In 2019, the Public Health Agency of Barcelona, Spain, was notified of a vaccine-derived poliovirus infection. The patient had an underlying common variable immunodeficiency and no signs of acute flaccid paralysis. We describe the ongoing coordinated response to contain the infection, which included compassionate-use treatment with Pocapavir.
Compassionate-use Pocapavir and immunoglobulin therapy for treatment of rituximab-associated enterovirus meningoencephalitis
J Neurovirol2022 Apr;28(2):329-334.PMID:34981437DOI:10.1007/s13365-021-01038-z.
A 71-year-old woman previously on rituximab treatment for rheumatoid arthritis presented with 2 years of progressive neurologic symptoms. She was found to have persistent hypogammaglobulinemia and B cell depletion despite rituximab discontinuation a year prior. MRI revealed diffuse meningeal enhancement along the entire neuroaxis. LP showed a CSF lymphocytic pleocytosis, elevated protein, and presence of enterovirus by PCR. The patient was hospitalized several times for progressive clinical and radiologic decline, though she had transient improvements following treatment with immunoglobulin therapy. Her CSF remained positive for enterovirus PCR for at least 12 months. Though two brain biopsies were non-diagnostic, pan-Enterovirus was ultimately identified using a high-throughput next-generation sequencing technique. She was treated with compassionate-use Pocapavir with clinical stabilization at 4-month follow-up; however, she expired 8 months later from a bacterial pneumonia.