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YH-53

YH-53
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YH-53

Catalog No. T9686Cas No. 1471484-62-4
YH-53 is a potent 3CLpro inhibitor, exhibiting K i values of 6.3 nM and 34.7 nM against SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, respectively. This peptidomimetic compound, characterized by its unique benzothiazolyl ketone structure, significantly inhibits SARS-CoV-2 replication, highlighting its potential in COVID-19 research [1] [2].
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
25 mg$1,6508-10 weeks
50 mg$2,1508-10 weeks
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Product Introduction

Bioactivity
Description
YH-53 is a potent 3CLpro inhibitor, exhibiting K i values of 6.3 nM and 34.7 nM against SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, respectively. This peptidomimetic compound, characterized by its unique benzothiazolyl ketone structure, significantly inhibits SARS-CoV-2 replication, highlighting its potential in COVID-19 research [1] [2].
In vitro
YH-53 demonstrates potent activity in reducing total RNA copies in VeroE6/TMPRSS2 cells, with efficiency increasing at concentrations between 1-25 μM over 24 hours [1]. Notably, YH-53 effectively inhibits viral proliferation of SARS-CoV-2 in Vero cells, particularly at a concentration of 10 μM over 48 hours, as evidenced by a cytopathic effect (CPE) assay, without exhibiting cytotoxicity at concentrations up to 100 μM [1]. Additionally, YH-53 moderately suppresses the activity of CYP1A2, CYP2D6, and CYP2C8 by 26.6%, 38.0%, and 66.4%, respectively, while not affecting CYP2C9 and CYP3A4 [1]. Moreover, it inhibits SARS-CoV 3CL pro with an IC50 of 0.74 μM [1]. This evidence underscores YH-53's potential as a selective and effective inhibitor for research in viral replication and metabolic enzyme interaction contexts.
In vivo
YH-53, administered to rats, demonstrates varied pharmacokinetic properties based on the route of administration. Intravenously at 0.1 mg/kg, YH-53 shows a half-life (T 1/2) of 2.97 hours, an area under the curve (AUC 0–∞) of 19.7 ng·h/mL, and a distribution volume (V d) of 3.51 L/kg. When given orally at 0.5 mg/kg, it exhibits a T 1/2 of 9.64 hours, an AUC 0–∞ of 3.49 ng·h/mL, and a maximum concentration (C max) of 1.08 ng/mL in rats. These findings provide useful insights into the compound's pharmacokinetics, indicating significant differences in half-life, distribution, and absorption rates between intravenous and oral administration in this animal model [1].
Chemical Properties
Molecular Weight575.68
FormulaC30H33N5O5S
Cas No.1471484-62-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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