ONO 5334

ONO 5334

中文名称ONO 5334
中文同义词化合物 T16394
英文名称ONO 5334
英文同义词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)-
CAS号868273-90-9
分子式C21H34N4O4S
分子量438.59
EINECS号
相关类别
Mol文件868273-90-9.mol
结构式ONO 5334 结构式

ONO 5334 性质

密度1.36±0.1 g/cm3(Predicted)
储存条件Store at -20°C
形态固体
酸度系数(pKa)7.06±0.40(Predicted)
颜色米白色至浅黄色

ONO 5334 用途与合成方法

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: Vero E6 cells
Concentration: 0.001 μM, 0.003 μM, 0.1 μM, 0.3 μM, 1 μM, 2.5 μM
Incubation Time: Pre-treated for 16 h and then cultured for 24 hours
Result: Inhibited SARS-COV-2 virus replication in a dose-dependent manner.

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: Monkey
Dosage: 0.3 mg/kg; 3 mg/kg
Administration: Oral administration; 7 consecutive days
Result: Reduced bone resorption markers but not bone formation markers in normal monkeys.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-108044ONO-53341 mg2000元
2024/04/30HY-108044ONO-533410 mM * 1 mLin DMSO4824元

ONO 5334 上下游产品信息

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