2. Anti-infection
  3. SARS-CoV
  4. YH-53

YH-53 is a potent 3CLpro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, 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.

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YH-53 Chemical Structure

YH-53 Chemical Structure

CAS No. : 1471484-62-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 550 In-stock
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10 mM * 1 mL in DMSO USD 550 In-stock
Solid
1 mg USD 200 In-stock
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1650 In-stock
50 mg USD 2600 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

YH-53 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

YH-53 is a potent 3CLpro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, 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[1][2].

IC50 & Target

Ki: 6.3 nM (SARS-CoV-1 3CLpro) and 34.7 nM (SARS-CoV-2 3CLpro)[1]
In Vitro

YH-53 (1-25 μM; for 24 h) efficiently reduces copies of total RNA with increased concentrations in VeroE6/TMPRSS2 cells[1].
? ? 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[1].
? ? YH-53 (10, 100 μM; for 24 h) has no cytotoxicity with a CC50 value of >100 μM in vero cells[1].
? ? 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[1].
? ? YH-53 inhibits SARS-CoV 3CLpro with an IC50 of 0.74 μM.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

YH-53 Related Antibodies

RT-PCR[1]

Cell 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 T1/2 of 2.97 hours, an AUC0–∞ of 19.7 ng?h/mL, a Vd of 3.51 L/kg in rats[1].
? ? YH-53 (0.5 mg/kg; oral) has a T1/2 of 9.64 hours, an AUC0–∞ of 3.49 ng?h/mL, a Cmax of 1.08 ng/mL in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats[1]
Dosage: 0.1 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 2.97 hours, an AUC0–∞ of 19.7 ng•h/mL, a Vd of 3.51 L/kg.
Molecular Weight

575.68

Formula

C30H33N5O5S
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (86.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7371 mL 8.6854 mL 17.3708 mL
5 mM 0.3474 mL 1.7371 mL 3.4742 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.61 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7371 mL 8.6854 mL 17.3708 mL 43.4269 mL
5 mM 0.3474 mL 1.7371 mL 3.4742 mL 8.6854 mL
10 mM 0.1737 mL 0.8685 mL 1.7371 mL 4.3427 mL
15 mM 0.1158 mL 0.5790 mL 1.1581 mL 2.8951 mL
20 mM 0.0869 mL 0.4343 mL 0.8685 mL 2.1713 mL
25 mM 0.0695 mL 0.3474 mL 0.6948 mL 1.7371 mL
30 mM 0.0579 mL 0.2895 mL 0.5790 mL 1.4476 mL
40 mM 0.0434 mL 0.2171 mL 0.4343 mL 1.0857 mL
50 mM 0.0347 mL 0.1737 mL 0.3474 mL 0.8685 mL
60 mM 0.0290 mL 0.1448 mL 0.2895 mL 0.7238 mL
80 mM 0.0217 mL 0.1086 mL 0.2171 mL 0.5428 mL
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YH-53 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YH-531471484-62-4YH53YH 53SARS-CoVSARS coronavirus3CLproSARS-CoV-1SARS-CoV-2replicationpeptidomimeticuniquebenzothiazolylketoneCOVID-19RNAVeroE6/TMPRSS2VeroInhibitorinhibitorinhibit

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