1. Cell Cycle/DNA Damage Anti-infection
  2. Deubiquitinase SARS-CoV
  3. GRL0617

GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome.

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GRL0617

GRL0617 構造式

CAS 番号 : 1093070-16-6

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
5 mg $90 在庫あり
10 mg $140 在庫あり
25 mg $260 在庫あり
50 mg $420 在庫あり
100 mg $670 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome[1].

IC50 & Target

IC50: 0.6 μM (SARS-CoV PLpro)[1]

Cellular Effect
Cell Line Type Value Description References
Vero CC50
500 3
Compound: 4; GRL0617
Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay
Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay
[PMID: 35620927]
Vero EC50
13.1 3
Compound: 25
Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
[PMID: 19645480]
Vero EC50
14.5 3
Compound: GRL0617
Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs
Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs
[PMID: 23231439]
Vero EC50
13.1 3
Compound: 25
Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
[PMID: 19645480]
Vero CC50
500 3
Compound: 4; GRL0617
Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay
Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay
[PMID: 35620927]
Vero EC50
14.5 3
Compound: GRL0617
Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs
Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs
[PMID: 23231439]
Vero C1008 EC50
10 3
Compound: 5
Antiviral activity against SARS coronavirus Urbani infected in monkey Vero E6 cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay
Antiviral activity against SARS coronavirus Urbani infected in monkey Vero E6 cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 32665808]
Vero CC50
500 3
Compound: 4; GRL0617
Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay
Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay
[PMID: 35620927]
Vero EC50
13.1 3
Compound: 25
Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
[PMID: 19645480]
Vero EC50
14.5 3
Compound: GRL0617
Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs
Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs
[PMID: 23231439]
Vero C1008 CC50
253.2 3
Compound: GRL0617
Cytotoxicity against african green monkey Vero E6 cells incubated for 48 hrs
Cytotoxicity against african green monkey Vero E6 cells incubated for 48 hrs
[PMID: 38871484]
Vero C1008 EC50
10 3
Compound: 5
Antiviral activity against SARS coronavirus Urbani infected in monkey Vero E6 cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay
Antiviral activity against SARS coronavirus Urbani infected in monkey Vero E6 cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 32665808]
体外実験

GRL0617 (0-50 μM; 48 h) exibits significantly antiviral activity in SARS-CoV infected Vero E6 cells[1].

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

Cell Viability Assay[1]

Cell Line: Vero E6 cells
Concentration: 0, 10, 20, 30, 40 and 50 μM
Incubation Time: 48 hours
Result: Showed significant antiviral activity in SARS-CoV infected Vero E6 cells with an EC50 value of 14.5 μM.
分子量

304.39

分子式

C20H20N2O

CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N[C@@H](C1=C2C=CC=CC2=CC=C1)C)C3=CC(N)=CC=C3C

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (410.66 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 3.2853 mL 16.4263 mL 32.8526 mL
5 mM 0.6571 mL 3.2853 mL 6.5705 mL
10 mM 0.3285 mL 1.6426 mL 3.2853 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 2.5 mg/mL (8.21 mM); Suspended solution; Need ultrasonic

  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (6.83 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.
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.
純度とドキュメンテーション
参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2853 mL 16.4263 mL 32.8526 mL 82.1315 mL
5 mM 0.6571 mL 3.2853 mL 6.5705 mL 16.4263 mL
10 mM 0.3285 mL 1.6426 mL 3.2853 mL 8.2131 mL
15 mM 0.2190 mL 1.0951 mL 2.1902 mL 5.4754 mL
20 mM 0.1643 mL 0.8213 mL 1.6426 mL 4.1066 mL
25 mM 0.1314 mL 0.6571 mL 1.3141 mL 3.2853 mL
30 mM 0.1095 mL 0.5475 mL 1.0951 mL 2.7377 mL
40 mM 0.0821 mL 0.4107 mL 0.8213 mL 2.0533 mL
50 mM 0.0657 mL 0.3285 mL 0.6571 mL 1.6426 mL
60 mM 0.0548 mL 0.2738 mL 0.5475 mL 1.3689 mL
80 mM 0.0411 mL 0.2053 mL 0.4107 mL 1.0266 mL
100 mM 0.0329 mL 0.1643 mL 0.3285 mL 0.8213 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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Inquiry Information

製品名:
GRL0617
製品番号:
HY-117043
数量:
MCE 日本正規代理店: