ONO-5334
Based on 2 publication(s) in Google Scholar
ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.
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 : 99.94%
- CAS 番号: 868273-90-9
- 分子式: C21H34N4O4S
- 分子量:438.58
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 ONO-5334
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生物活性
製品説明
IC50 & Target
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cathepsin K |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero C1008 | EC50 |
0.5 μM
Compound: ONO 5334
|
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
|
[PMID: 32511357] |
| Vero C1008 | EC50 |
0.5 μM
Compound: ONO 5334
|
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
|
10.1101/2020.04.16.044016 |
体外実験
ONO-5334 has inhibitory effects on human cathepsin S, human cathepsin L, human cathepsin B, porcine calpain Ι and porcine calpain II with Ki values of 0.83 nM, 1.7 nM, 32 nM, 82 nM and 69 nM, respectively[1].ONO-5334 (0.1-1 μM; 24 hours) suppresses human osteoclast-mediated bone resorption. It potently reduces osteoclast-mediated release of CTX from bone slices as a dose dependent manner[1].ONO-5334 (0-10 μM; pre-treated for 16 h) inhibits antiviral activities in a discernable dose-dependent manner in Vero E6 cells by designed to capture multicycle replication, exhibiting an EC50 value of 0.5 μM[2]/
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Vero E6 cells
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Concentration:0.001 μM, 0.003 μM, 0.1 μM, 0.3 μM, 1 μM, 2.5 μM
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Incubation Time:Pre-treated for 16 h and then cultured for 24 hours
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Result:Inhibited SARS-COV-2 virus replication in a dose-dependent manner.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Monkey[1]
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Dosage:0.3 mg/kg; 3 mg/kg
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Administration:Oral administration; 7 consecutive days
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Result:Reduced bone resorption markers but not bone formation markers in normal monkeys.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 868273-90-9
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性状 Solid
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分子量 438.58
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分子式 C21H34N4O4S
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Color Off-white to light yellow
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SMILES
O=C(C(N/N=C(SC[C@H]1C)/N1C)=O)[C@H](C2CCOCC2)NC(C3CCCCCC3)=O
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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 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390 -
Sci Rep
Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]2022 Jul 16;12(1):12197. PMID: 35842458
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (114.00 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2801 mL | 11.4004 mL | 22.8009 mL | 57.0021 mL |
| 5 mM | 0.4560 mL | 2.2801 mL | 4.5602 mL | 11.4004 mL | |
| 10 mM | 0.2280 mL | 1.1400 mL | 2.2801 mL | 5.7002 mL | |
| 15 mM | 0.1520 mL | 0.7600 mL | 1.5201 mL | 3.8001 mL | |
| 20 mM | 0.1140 mL | 0.5700 mL | 1.1400 mL | 2.8501 mL | |
| 25 mM | 0.0912 mL | 0.4560 mL | 0.9120 mL | 2.2801 mL | |
| 30 mM | 0.0760 mL | 0.3800 mL | 0.7600 mL | 1.9001 mL | |
| 40 mM | 0.0570 mL | 0.2850 mL | 0.5700 mL | 1.4251 mL | |
| 50 mM | 0.0456 mL | 0.2280 mL | 0.4560 mL | 1.1400 mL | |
| 60 mM | 0.0380 mL | 0.1900 mL | 0.3800 mL | 0.9500 mL | |
| 80 mM | 0.0285 mL | 0.1425 mL | 0.2850 mL | 0.7125 mL | |
| 100 mM | 0.0228 mL | 0.1140 mL | 0.2280 mL | 0.5700 mL |