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LY1

目录号 : GC71194

LY1是一种针对严重急性呼吸系统综合征冠状病毒2型PLpro和Mpro的强效、选择性和共价抑制剂,Mpro C145A蛋白和PLpro C111A蛋白的Kd值分别为1.5μM和2.3μM。

LY1 Chemical Structure

Cas No.:2883813-32-7

规格 价格 库存 购买数量
1 mg
¥1,395.00
现货
5 mg
¥3,186.00
现货
10 mg
¥5,094.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

LY1 is a potent, selective and covalent inhibitor against both SARS-CoV-2 PLpro and Mpro with Kd values of 1.5 μM and 2.3 μM for Mpro C145A protein and PLpro C111A protein, respectively. LY1 potent against the viral proteases, with IC50s of 0.12 μM and 0.99 μM against Mpro and PLpro. LY1 shows high selectivity over other kinases, human proteases and metalloenzyme.

In SARS-CoV-2-infected Vero E6 cells, LY1 causes a dramatic reduction in the viral nucleoprotein (NP) levels with 5 μM. A 99.99% reduction in the viral RdRP RNA levels is observed with 15 μM LY1[1].
LY1 against cathepsin B and cathepsin L with the IC50 values of 8.8 μM and 2.2 μM, respectively[1].

In the 8 week toxicity study, rats are orally administered with LY1 up to 300 mg/kg for 4 weeks and then recovered for another 4 weeks; no significant change in body weight and food consumption is observed in any group[1].

References:
[1]. Wenying Yu, et al. Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2. J Med Chem. 2022 Dec 22;65(24):16252-16267.

Chemical Properties

Cas No. 2883813-32-7 SDF
分子式 C20H19ClN4O3S 分子量 430.91
溶解度 DMSO : 50 mg/mL (116.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 4°C, protect from light, stored under nitrogen
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.3207 mL 11.6034 mL 23.2067 mL
5 mM 0.4641 mL 2.3207 mL 4.6413 mL
10 mM 0.2321 mL 1.1603 mL 2.3207 mL
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