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• 產品描述： Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses

• 靶點： IC50: 2 nM (influenza virus neuraminidase);InfluenzaVirus;DrugMetabolite

• 體內研究：
  Oseltamivir (0.1, 1, or 10 mg/kg/day, twice daily by oral gavage) produces a dose-dependent antiviral effect against Vietnam/1203/04 (VN1203/04) virus. The 5-day regimen at 10 mg/kg/day protects 50% of mice; deaths in this treatment group are delayed and indicated the replication of residual virus after the completion of treatment. Eight-day regimens improved Oseltamivir efficacy, and dosages of 1 and 10 mg/kg/day significantly reduced virus titers in organs and provided 60% and 80% survival rates, respectively. In the pharmacokinetic study, after the oral administration of 1,000 mg/kg Oseltamivir, peak plasma concentrations are reached at 2 h postdose for Oseltamivir and 8 h for Oseltamivir carboxylate (OC). Rats are exposed to Oseltamivir over the whole sampling interval and had a ~2.7-fold-higher rate of exposure to OC than Oseltamivir. In CSF, peak concentrations are reached at 2 h postdose for Oseltamivir and 6 h for OC. CSF/plasma exposure ratios (AUC0-8 h) are ~0.07 for Oseltamivir and 0.007 for OC. In perfused brain samples, peak concentrations are reached at 8 h postdose for Oseltamivir and 6 h for OC. Brain/plasma exposure ratios (AUC0-8 h) of ~0.12 for Oseltamivir and 0.01 for OC are recorded. Corresponding CSF/brain exposure ratios ranged between ~0.55 and 0.64 for both analytes. A further group of animals that received a single oral administration of Oseltamivir at a lower dose produced similar results.

• 參考文獻：
  1. Li W, et al. Identification of GS 4104 as an orally bioavailable prodrug of the influenza virus neuraminidase inhibitor GS 4071. Antimicrob Agents Chemother. 1998 Mar;42(3):647-53. 2. Ghosh GC, et al. Oseltamivir carboxylate, the active metabolite of oseltamivir phosphate (Tamiflu), detected in sewage discharge and river water in Japan. Environ Health Perspect. 2010 Jan;118(1):103-7. 3. Ferraris O, et al. Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice. Antiviral Res. 2005 Oct;68(1):43-8. 4. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants.Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8. 5. Yen HL, et al. Virulence may determine the necessary duration and dosage of oseltamivir treatment for highly pathogenic A/Vietnam/1203/04 influenza virus in mice. J Infect Dis. 2005 Aug 15;192(4):665-72. 6. Hoffmann G, et al. Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system. Antimicrob Agents Chemother. 2009 Nov;53(11):4753-61.

• 溶解性： DMSO  :  ≥  230  mg/mL  (808.86  mM)    H2O  :  125  mg/mL  (439.60  mM;  Need  ultrasonic)

• 保存條件： 2-8℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	3.517 ml	17.584 ml	35.168 ml
  5 mM	0.703 ml	3.517 ml	7.034 ml
  10 mM	0.352 ml	1.758 ml	3.517 ml
  50 mM	0.07 ml	0.352 ml	0.703 ml

• 注意：部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

• 5. [IF=12.7] Zhongyuan Li et al."Development of a virus-based affinity ultrafiltration method for screening virus-surface-protein-targeted compounds from complex matrixes: Herbal medicines as a case study."JOURNAL OF MEDICAL VIROLOGY".2024 Mar;96(3):e29517

• 4. [IF=3] Xiaofan Fan et al."Screening and identification of neuraminidase inhibitors from Baphicacanthus cusia by a combination of affinity ultrafiltration, HPLC-MS/MS, molecular docking, and fluorescent techniques."JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGI

• 3. [IF=4.759] Yichao Zang et al."Development of a thin-layer chromatography bioautographic assay for neuraminidase inhibitors hyphenated with electrostatic field induced spray ionisation-mass spectrometry for identification of active Isatis indigotica root compounds."J

• 2. [IF=4.946] Lai Yanni et al."3D-quantitative structure–activity relationship and antiviral effects of curcumin derivatives as potent inhibitors of influenza H1N1 neuraminidase."Arch Pharm Res. 2020 May;43(5):489-502

• 1. Zang, Yichao, et al. "Development of a thin-layer chromatography bioautographic assay for neuraminidase inhibitors hyphenated with electrostatic field induced spray ionisation-mass spectrometry for identification of active Isatis indigotica root compounds.

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本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系，公式為：

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *