ONO 5334
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- CAS号:
- 868273-90-9
- 英文名:
- ONO 5334
- 英文别名:
- ONO 5334;ONO5334,ONO 5334;2H-Pyran-4-propanoic acid, β-[(cycloheptylcarbonyl)amino]tetrahydro-α-oxo-, (2Z)-2-[(4R)-3,4-dimethyl-2-thiazolidinylidene]hydrazide, (βS)-
- 中文名:
- ONO 5334
- 中文别名:
- 化合物 T16394
- CBNumber:
- CB53146346
- 分子式:
- C21H34N4O4S
- 分子量:
- 438.59
- MOL File:
- 868273-90-9.mol
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ONO 5334化学性质
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密度:
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1.36±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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形态:
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Solid
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酸度系数(pKa):
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7.06±0.40(Predicted)
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颜色:
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Off-white to light yellow
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ONO 5334性质、用途与生产工艺
ONO-5334 是一种强效、选择性和口服活性的组织蛋白酶 K (cathepsin K) 抑制剂,对人、兔和大鼠组织蛋白酶 K 的作用值分别为 0.10 nM、0.049 nM 和 0.85 nM。ONO-5334 是一种有效的抗 SAR-COV-2 病毒活性的抗病毒化合物,其 EC50 值为 500 nM。ONO-5334 有潜力用于骨质疏松症以及 COVID-19 的相关研究。
Ki: 0.10 nM (human cathepsin K)Ki: 0.049 nM (rabbit cathepsin K)Ki: 0.85 nM (rat cathepsin K)
ONO-5334 has inhibitory effects on human cathepsin S, human cathepsin L, human cathepsin B, porcine calpain Ι and porcine calpain II with
K
i
values of 0.83 nM, 1.7 nM, 32 nM, 82 nM and 69 nM, respectively.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.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 EC
50
value of 0.5 μM/
Cell Viability Assay
Cell Line:
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Vero E6 cells
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Concentration:
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0.001 μM, 0.003 μM, 0.1 μM, 0.3 μM, 1 μM, 2.5 μM
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Incubation Time:
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Pre-treated for 16 h and then cultured for 24 hours
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Result:
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Inhibited SARS-COV-2 virus replication in a dose-dependent manner.
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ONO-5334 (oral administration; 0.12-15 mg/kg; single dose) can dose-dependently reduce PTHrP-induced increase in plasma calcium with significant effect (86% reduction) at 15 mg/kg. It also reduces PTHrP-induced increase in plasma CTX level in TPTX rats by 90% at 15 mg/kg.ONO-5334 (oral administration; 0.3-30 mg/kg; 7 consecutive days) at 3 mg/kg or 30 mg/kg significantly decreases CTX (a bone resorption marker) concentration. On day 7, the reduction in serum CTX concentration by ONO-5334 at 3 mg/kg and 30 mg/kg was 62% and 79%, respectively.
Animal Model:
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Monkey
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Dosage:
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0.3 mg/kg; 3 mg/kg
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Administration:
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Oral administration; 7 consecutive days
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Result:
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Reduced bone resorption markers but not bone formation markers in normal monkeys.
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ONO 5334
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | HY-108044 | ONO-5334 | | 1 mg | 2000元 |
2024/08/19 | HY-108044 | ONO-5334 | | 10 mM * 1 mLin DMSO | 4824元 |
868273-90-9, ONO 5334 相关搜索:
- 化合物 T16394
- 868273-90-9
- 2H-Pyran-4-propanoic acid, β-[(cycloheptylcarbonyl)amino]tetrahydro-α-oxo-, (2Z)-2-[(4R)-3,4-dimethyl-2-thiazolidinylidene]hydrazide, (βS)-
- ONO5334,ONO 5334
- ONO 5334