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

For research use only. We do not sell to patients.

LY1 Chemical Structure

LY1 Chemical Structure

CAS No. : 2883813-32-7

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1 mg USD 155 In-stock
5 mg USD 354 In-stock
10 mg USD 566 In-stock
25 mg USD 1188 In-stock
50 mg USD 1900 In-stock
100 mg USD 3046 In-stock
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Based on 1 publication(s) in Google Scholar

LY1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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[1].

IC50 & Target

Kd: 1.5 μM (Mpro C145A protein) and 2.3 μM (PLpro C111A protein)[1].
IC50: 0.12 μM (Mpro protease) and 0.99 μM (PLpro protease)[1].
In Vitro

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].

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

LY1 Related Antibodies
In Vivo

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].

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

430.91

Formula

C20H19ClN4O3S
CAS No.
Appearance

Solid

Color

Pale purple to purple

SMILES

O=C1C=C(C2=NS(=O)(C3=C2C1=CC=C3)=O)NC4=C(C=CC=C4)N5CCNCC5.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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 (protect from light, stored under nitrogen). 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: ≥ 2.5 mg/mL (5.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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 (protect from light, stored under nitrogen). 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 2.3207 mL 11.6034 mL 23.2067 mL 58.0168 mL
5 mM 0.4641 mL 2.3207 mL 4.6413 mL 11.6034 mL
10 mM 0.2321 mL 1.1603 mL 2.3207 mL 5.8017 mL
15 mM 0.1547 mL 0.7736 mL 1.5471 mL 3.8678 mL
20 mM 0.1160 mL 0.5802 mL 1.1603 mL 2.9008 mL
25 mM 0.0928 mL 0.4641 mL 0.9283 mL 2.3207 mL
30 mM 0.0774 mL 0.3868 mL 0.7736 mL 1.9339 mL
40 mM 0.0580 mL 0.2901 mL 0.5802 mL 1.4504 mL
50 mM 0.0464 mL 0.2321 mL 0.4641 mL 1.1603 mL
60 mM 0.0387 mL 0.1934 mL 0.3868 mL 0.9669 mL
80 mM 0.0290 mL 0.1450 mL 0.2901 mL 0.7252 mL
100 mM 0.0232 mL 0.1160 mL 0.2321 mL 0.5802 mL
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LY1 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:

LY12883813-32-7LY 1LY-1SARS-CoVSARS coronavirusPLproMproSARS-CoV-2covalentviral proteasesInhibitorinhibitorinhibit

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