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H2L 5765834

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Catalog No. T22834Cas No. 420841-84-5

H2L 5765834 is a lysophosphatidic acid receptors antagonist

H2L 5765834

H2L 5765834

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Purity: 99.47%
Catalog No. T22834Cas No. 420841-84-5
H2L 5765834 is a lysophosphatidic acid receptors antagonist
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$56-In Stock
5 mg$122-In Stock
10 mg$197-In Stock
25 mg$372-In Stock
50 mg$553-In Stock
100 mg$787-In Stock
1 mL x 10 mM (in DMSO)$133-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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.
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Purity:99.47%
Appearance:Solid
Color:White to Yellow
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Product Introduction

H2L 5765834 AI Summary
H2L 5765834 demonstrates antagonist activity at the LPA1, LPA3, and LPA5 receptors in rat RH7777 cells, showing significant binding affinities with Ki values of 48.0 nM for LPA1, 230.0 nM for LPA3, and 292.0 nM for LPA5. The compound effectively inhibits LPA-induced calcium responses with IC50 values of 94.0 nM at LPA1, 752.0 nM at LPA3, and 463.0 nM at LPA5. In addition to its receptor antagonism, H2L 5765834 exhibits antiviral activity against SARS-CoV-2. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells at 10 µM over 48 hours, with an inhibition rate of -5.66%. The compound also demonstrates inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM, showing inhibition percentages of 21.89% and 31.72% in FRET assays. Moreover, it reduces cytotoxicity in VERO-6 cells at 10 µM after 48 hours with an inhibition rate of approximately 0.78%. Additionally, H2L 5765834 functions as an inhibitor of the human HDAC6 enzyme, achieving -41.12% inhibition with a commercial peptide substrate and 23.52% with a custom peptide substrate..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
H2L 5765834 is a lysophosphatidic acid receptors antagonist
Targets&IC50
LPA5 receptor:463 nM (IC50), LPA3 receptor:752 nM (IC50), LPA1 receptor:94 nM (IC50)
Chemical Properties
Molecular Weight404.33
FormulaC21H12N2O7
Cas No.420841-84-5
SmilesOC(=O)c1ccc2C(=O)N(C(=O)c2c1)c1cccc(Oc2ccc(cc2)[N+]([O-])=O)c1
Relative Density.1.544 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (136.03 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4732 mL12.3661 mL24.7323 mL123.6614 mL
5 mM0.4946 mL2.4732 mL4.9465 mL24.7323 mL
10 mM0.2473 mL1.2366 mL2.4732 mL12.3661 mL
20 mM0.1237 mL0.6183 mL1.2366 mL6.1831 mL
50 mM0.0495 mL0.2473 mL0.4946 mL2.4732 mL
100 mM0.0247 mL0.1237 mL0.2473 mL1.2366 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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