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LY1

カタログ番号GC71194 Copy One-Click Copy Product Info

LY1 は重症急性呼吸器症候群コロナウイルス2型PLproとMproに対する強力、選択性と共有結合抑制剤であり、Mpro C 145 Aタンパク質とPLpro C 111 Aタンパク質のKd値はそれぞれ1.5μMと2.3μMである。

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LY1 化学構造

Cas No.: 2883813-32-7

サイズ 価格 在庫数 個数
1 mg
$140.00
在庫あり
5 mg
$319.00
在庫あり
10 mg
$509.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.



Description of LY1

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 of LY1

Cas No. 2883813-32-7 SDF
Formula C20H19ClN4O3S M.Wt 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) Storage 4°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of LY1

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3207 mL 11.6034 mL 23.2067 mL
5 mM 464.1 μL 2.3207 mL 4.6413 mL
10 mM 232.1 μL 1.1603 mL 2.3207 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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