Laninamivir
(Synonyms: 拉尼米韦,R 125489) 目录号 : GC65069
Laninamivir (R 125489) 是一种有效的流感神经氨酸酶 (NA) 抑制剂，其对流感病毒 H12N5 NA (N5)，pH1N1 N1 NA (p09N1) 和 A/RI/5+/1957 H2N2 N2 (p57N2) 的 IC50 分别为 0.90 nM、1.83 nM 和 3.12 nM。
Cas No.:203120-17-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively[1].
Laninamivir (R 125489) inhibits efficiently common oseltamivir-resistant viruses, including those with the ubiquitous His274Tyr substitution[1].Laninamivir (R 125489) is potent against p57N2, p09N1 and N5 with a similar binding mode to Zanamivir[1].
[1]. Vavricka CJ, et al. Structural and functional analysis of laninamivir and its octanoate prodrug reveals group specific mechanisms for influenza NA inhibition. PLoS Pathog. 2011 Oct;7(10):e1002249.
| Cas No. | 203120-17-6 | SDF | Download SDF |
| 别名 | 拉尼米韦,R 125489 | ||
| 分子式 | C13H22N4O7 | 分子量 | 346.34 |
| 溶解度 | Water : 5 mg/mL (14.44 mM; Need ultrasonic) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8873 mL | 14.4367 mL | 28.8734 mL |
| 5 mM | 0.5775 mL | 2.8873 mL | 5.7747 mL |
| 10 mM | 0.2887 mL | 1.4437 mL | 2.8873 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。
Laninamivir octanoate: a new long-acting neuraminidase inhibitor for the treatment of influenza
Expert Rev Anti Infect Ther 2011 Oct;9(10):851-7.PMID:21973296DOI:10.1586/eri.11.112.
Oseltamivir and zanamivir are well-established and well-researched drugs for the treatment of influenza in Japan and the rest of the world. A new neuraminidase inhibitor, Laninamivir octanoate, has been approved for use in Japanese clinics. Laninamivir octanoate is an inhaled drug with unique characteristics. The inhaled Laninamivir octanoate is converted into its active form, Laninamivir, in the lungs where a high concentration persists for a long period of time. The concentration of Laninamivir exceeds the level necessary for influenza virus replication inhibition for at least 5 days, thus influenza can be treated with a single administration. The drug is delivered using one device requiring four inhalations for children and two devices requiring eight inhalations for adults. Clinical trials have shown comparable efficacy for Laninamivir octanoate and oseltamivir. Laninamivir octanoate also displayed a sufficient antiviral effect to treat infection with H275Y-mutated oseltamivir-resistant virus. Laninamivir octanoate has displayed clinical efficacy comparable to that of oseltamivir and zanamivir against the H1N1 pandemic influenza strain from 2009, seasonal H3N2 influenza and influenza B viruses. The prophylactic efficacy of Laninamivir octanoate has been shown in animal models. The effectiveness of Laninamivir against the highly pathogenic avian influenza virus H5N1 has also been shown in vitro and in animal models. A major clinical benefit of this drug is that the single administration is very convenient for both the patient and doctor, which leads to improved compliance. Furthermore, this drug shows promise for the treatment of influenza in future pandemics.
Laninamivir-induced ischemic enterocolitis: A case report
World J Clin Cases 2022 Mar 26;10(9):2864-2870.PMID:35434102DOI:10.12998/wjcc.v10.i9.2864.
Background: Neuraminidase inhibitor-associated acute hemorrhagic colitis is rare. We report a case of ischemic enterocolitis that was likely caused by Laninamivir. Case summary: A 54-year-old female patient with influenza type A was administered 40 mg of Laninamivir via inhalation once. On the same day, the patient experienced bloody stools and lower abdominal pain. A contrast-enhanced abdominal computed tomography showed edema-like changes from the descending colon to the sigmoid colon, which suggested ischemic enterocolitis. Conclusion: We treated a patient with ischemic enterocolitis caused by Laninamivir, a rare but similar symptom following the administration of oseltamivir.
Laninamivir and its prodrug, CS-8958: long-acting neuraminidase inhibitors for the treatment of influenza
Antivir Chem Chemother 2010;21(2):71-84.PMID:21107016DOI:10.3851/IMP1688.
Oseltamivir and zanamivir are currently licensed worldwide for influenza treatment and chemoprophylaxis. Both drugs require twice-daily administration for 5 days for treatment. A new influenza drug, Laninamivir (code name R-125489), and its prodrug form, CS-8958 (Laninamivir octanoate or Laninamivir prodrug), which are long-acting neuraminidase inhibitors, are introduced in this review. Laninamivir potently inhibited the neuraminidase activities of various influenza A and B viruses, including subtypes N1-N9, pandemic (2009) H1N1 virus, highly pathogenic avian influenza (HPAI) H5N1 viruses and oseltamivir-resistant viruses. Because of the long retention of Laninamivir in mouse lungs after an intranasal administration of CS-8958, therapeutic administration of a single dose of CS-8958 showed superior efficacy to repeated administrations of zanamivir or oseltamivir in animal infection models for influenza A and B viruses. These include pandemic (2009) H1N1 virus and HPAI H5N1 virus. Prophylactic single administration of CS-8958, as early as 7 days prior to infection, also showed superior efficacy. Finally, the potential of a single inhalation of CS-8958 for influenza patients was demonstrated by clinical studies, and CS-8958 has been approved and is commercially available as Inavir(®) (Daiichi Sankyo Co., Ltd, Tokyo) in Japan.
Safety of the long-acting neuraminidase inhibitor Laninamivir octanoate hydrate in post-marketing surveillance
Int J Antimicrob Agents 2012 Nov;40(5):381-8.PMID:22871369DOI:10.1016/j.ijantimicag.2012.06.017.
Laninamivir octanoate hydrate (Laninamivir) is a long-acting neuraminidase inhibitor (NAI) that completes treatment with only a single inhalation. It was launched in Japan in October 2010 as an anti-influenza agent. A post-marketing surveillance study was conducted in the 2010/2011 influenza season to assess the safety of this drug in clinical settings. Adverse drug reactions (ADRs) were observed in 50 patients (59 events) out of 3542 patients subjected to safety evaluation (incidence 1.41%). Commonly reported ADRs were psychiatric disorders (abnormal behaviour, etc.), gastrointestinal disorders (diarrhoea, nausea, etc.) and nervous system disorders (dizziness, etc.), with incidences of 0.48% (n=17), 0.45% (n=16) and 0.17% (n=6), respectively. No serious ADRs occurred. ADRs usually emerged on the day on which Laninamivir was inhaled (52.5%) and ADRs emerged within 3 days after inhalation in >90% of adversely affected patients. ADRs resolved or improved within 3 days in >85% of patients. The incidence of adverse events involving abnormal behaviour was 3.1% (30/959) among patients <10 years of age, 0.7% (8/1088) among patients aged 10-19 years, 0.1% (2/1431) among adult patients aged 20-64 years and 0.0% (0/64) among patients aged ≥65 years. It was confirmed that Laninamivir is unlikely to cause delayed ADRs or a prolonged duration of ADRs despite this drug being a long-acting NAI. Furthermore, the incidence of ADRs was not found to have increased compared with that observed during clinical trials, and the types of ADR observed during this study were similar to those previously observed. Thus, Laninamivir octanoate hydrate was confirmed to have no noticeable problem with safety.
Inhaled Laninamivir Octanoate as Prophylaxis for Influenza in Children
Pediatrics 2016 Dec;138(6):e20160109.PMID:27940664DOI:10.1542/peds.2016-0109.
Background: A single 20-mg dose of inhaled Laninamivir octanoate is an effective treatment of influenza. However, the efficacy of Laninamivir octanoate for the prevention of influenza in children <10 years of age has not yet been established. Methods: We conducted a double-blind, multicenter, randomized, placebo-controlled study to determine whether the efficacy of a single 20-mg dose of inhaled Laninamivir octanoate to prevent the development of influenza was superior to that of placebo as prophylaxis for influenza in pediatric (<10 years) household members of index cases. Eligible subjects without influenza, in contact with an influenza-infected index case living in the same household, were blindly randomly assigned in a 1:1 ratio to receive 20 mg of Laninamivir octanoate or placebo. The primary end point was the proportion of subjects who developed clinical influenza during a 10-day period. Results: A total of 343 subjects were randomly assigned, with 341 subjects included in the full analysis set for the primary analysis. The proportions of subjects who developed clinical influenza were 11% (18/171) in the Laninamivir octanoate group and 19% (33/170) in the placebo group (P = .02). The relative risk reduction was 45.8% (95% confidence interval, 7.5% to 68.2%). The incidence of adverse events was similar in both groups. Conclusions: A single 20-mg dose of inhaled Laninamivir octanoate was effective and well tolerated as prophylaxis for influenza.