计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
YH-53 is a potent 3CL pro inhibitor with K i values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CL pro and SARS-CoV-2 3CL pro , respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research
In Vitro
YH-53 (1-25 μM; for 24 h) efficiently reduces copies of total RNA with increased concentrations in VeroE6/TMPRSS2 cells. YH-53 (1, 5, 10, 15, 20, 25 μM; for 48 h) with 10 μM completely blocks the viral proliferation against SARS-CoV-2 were examined by a cytopathic effect (CPE) assay in Vero cells. YH-53 (10, 100 μM; for 24 h) has no cytotoxicity with a CC 50 value of >100 μM in vero cells. YH-53 (10 μM) moderately inhibits CYP1A2, CYP2D6, and CYP2C8 (26.6%, 38.0%, 66.4%, respectively). YH-53 has no inhibition on CYP2C9 and CYP3A4. YH-53 inhibits SARS-CoV 3CL pro with an IC 50 of 0.74 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: VeroE6/TMPRSS2 cells Concentration: 1, 5, 10, 15, 20, 25 μM Incubation Time: 24 hours Result: Efficiently reduced copies of total RNA.
In Vivo
YH-53 (0.1 mg/kg; iv) has a T 1/2 of 2.97 hours, an AUC 0–∞ of 19.7 ng•h/mL, a V d of 3.51 L/kg in rats . YH-53 (0.5 mg/kg; oral) has a T 1/2 of 9.64 hours, an AUC 0–∞ of 3.49 ng•h/mL, a C max of 1.08 ng/mL in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Rats Dosage: 0.1 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Had a T 1/2 of 2.97 hours, an AUC 0–∞ of 19.7 ng•h/mL, a V d of 3.51 L/kg.
Form:Solid
IC50& Target:Ki: 6.3 nM (SARS-CoV-1 3CL pro ) and 34.7 nM (SARS-CoV-2 3CL pro )
规格
规格或纯度
≥98%
英文名称
YH-53
生化机理
YH-53 是一种强效的 3CL pro 抑制剂，对 SARS-CoV-1 3CL pro 和 SARS-CoV-2 3CL pro 的 K i 值分别为 6.3 nM 和 34.7 nM。YH-53 能强烈阻断 SARS-CoV-2 的复制。YH-53 是一种具有独特苯并噻唑酮的拟肽化合物。
储存条件
-20°C储存
运输条件
超低温运输
纯度
≥98%
名称和识别符
分子类型
小分子
Smiles
COC1=C2C(NC(C(N[C@@H](CC(C)C)C(N[C@@H](C[C@H]3C(NCC3)=O)C(C4=NC5=CC=CC=C5S4)=O)=O)=O)=C2)=CC=C1
分子量
575.68
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 50 mg/mL (86.85 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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