貨號	規格	價格	上海	北京	武漢	南京
S80494-5mg	99.2%	￥240.00 S80494-5mg ￥240.00 現貨	3 3	-	-	-
S80494-10mg	99.2%	￥400.00 S80494-10mg ￥400.00 現貨	1 1	-	-	-
S80494-25mg	99.2%	￥770.00 S80494-25mg ￥770.00 現貨	7 7	-	-	-
S80494-50mg	99.2%	￥1320.00 S80494-50mg ￥1320.00 現貨	6 6	-	-	-

產品介紹

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

產品描述：

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。

參考文獻(6篇)

6. [IF=4.8] Zhongyuan Li et al."Combining virus-based affinity ultrafiltration method with serum pharmacochemistry to identify the antiviral pharmacodynamic substances in licorice."JOURNAL OF ETHNOPHARMACOLOGY.2024 Oct;:118978 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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OSELTAMIVIR ACID