Ziresovir
Based on 5 publication(s) in Google Scholar
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.33%
- CAS 番号: 1422500-60-4
- 分子式: C22H25N5O3S
- 分子量:439.53
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Ziresovir
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Cell Proliferation/Viability Assay
生物活性
RSV F protein (respiratory syncytial virus fusion protein)[1] EC50: 3 nM (RSV F)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEp-2 | CC50 |
>100 μM
Compound: RO-0529; AK0529
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Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 5 days by CCK-8 assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 5 days by CCK-8 assay
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[PMID: 31194544] |
Ziresovir shows different efficacy in Wild Type (WT) and Mutant Strains RSV with EC50/EC90 values (μM) of 0.003/0.005 (WT), 2.1/10.0 (D486N), and >10/>10 (D489A), respectively[1].
RO-0529 (100 nM; 4 d) inhibits RSV F protein-induced cell–cell fusion process, and suppresses the syncytia formation induced by the RSV F protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ziresovir (10 mg/kg; p.o.; single dose) exhibits good oral exposure and bioavailability with F(%) of 32% in male Wistar-Han rats[1].
Ziresovir (150 mg/kg; p.o.; single dose) demonstrates a high tissue distribution to lung than plasma in CD-1 Mice[1].
Pharmacokinetics of Ziresovir in male Wistar-Han rats[1]
| Dose (mg/kg) | AUC0-24h(p.o.) (ng·h/mL) | CL (mL/min/kg) | T1/2(i.v.) (h) | Vss (L/kg) | F (%) |
| 2 mg/kg (iv) or 10 mg/kg (po) | 906 | 58 | 1.2 | 3.9 | 32 |
| Dose (mg/kg) | AUC0-24h(p.o.) (μg·h/L) | tissue/lasma AUC0-24h ratio (μg·h/L) | T1/2 (h) | Tmax (h) | Cmax (μg/L) |
| plasma | 8,380 | 1 | 1.02 | 0.25 | 5090 |
| lung | 72,400 | 8.6 | 3.31 | 1 | 22700 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice infected by RSV[1]
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Dosage:12.5 mg/kg, 50 mg/kg
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Administration:Oral gavage; twice daily; 4 days
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Result:Resulted >1 log unit of viral titer reduction in the lung of infected mice at the dose level as low as 12.5 mg/kg.
Reduced viral titer to 1.9 log units compared to vehicle at 50 mg/kg dose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1422500-60-4
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性状 Solid
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分子量 439.53
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分子式 C22H25N5O3S
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Color White to off-white
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SMILES
NC1(COC1)CNC2=NC(N(CC3)CC4=CC=CC=C4S3(=O)=O)=NC5=C2C=C(C)C=C5
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別名
AK0529; RO-0529
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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mBio
A new mechanism of respiratory syncytial virus entry inhibition by small-molecule to overcome K394R-associated resistance. [Abstract]2024 Aug 20:e0138524. PMID: 39162560 -
J Virol
Molecular mechanism of resistance to lonafarnib conferred by mutations in the cysteine-rich region of respiratory syncytial virus fusion glycoprotein and discovery of a lonafarnib-derived antiviral PROTAC. [Abstract]2025 Dec 9:e0148725. PMID: 41364004 -
J Infect Dis
EDP-938 Has a High Barrier to Resistance in Healthy Adults Experimentally Infected with Respiratory Syncytial Virus. [Abstract]2024 Oct 23:jiae471. PMID: 39441691 -
J Virol
Mechanism of Cross-Resistance to Fusion Inhibitors Conferred by the K394R Mutation in Respiratory Syncytial Virus Fusion Protein. [Abstract]2021 Sep 27;95(20):e0120521. PMID: 34379500
Ziresovir purchased from MedChemExpress. Usage Cited in: J Virol. 2021 Sep 27;95(20):e0120521. [Abstract]
Cooperative effects of escape mutations for RSV F inhibitors on resistance. HEK293T cells were transfected with plasmids harboring escape mutations for RSV F inhibitors. At 24 h posttransfection, the cells were treated with AK-0529 (Ziresovir). Cell-cell fusion activity was determined at 72 h posttransfection.
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Viruses
A Pseudovirus-Based Entry Assay to Evaluate Neutralizing Activity against Respiratory Syncytial Virus. [Abstract]2023 Jul 14;15(7):1548. PMID: 37515234
溶剤 & 溶解度
DMSO : 125 mg/mL (284.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2752 mL | 11.3758 mL | 22.7516 mL | 56.8789 mL |
| 5 mM | 0.4550 mL | 2.2752 mL | 4.5503 mL | 11.3758 mL | |
| 10 mM | 0.2275 mL | 1.1376 mL | 2.2752 mL | 5.6879 mL | |
| 15 mM | 0.1517 mL | 0.7584 mL | 1.5168 mL | 3.7919 mL | |
| 20 mM | 0.1138 mL | 0.5688 mL | 1.1376 mL | 2.8439 mL | |
| 25 mM | 0.0910 mL | 0.4550 mL | 0.9101 mL | 2.2752 mL | |
| 30 mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.8960 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5688 mL | 1.4220 mL | |
| 50 mM | 0.0455 mL | 0.2275 mL | 0.4550 mL | 1.1376 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9480 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2844 mL | 0.7110 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2275 mL | 0.5688 mL |
Ziresovir 関連分類
HY-109142 関連分類
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