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AM966

🥰Excellent
Catalog No. T4278Cas No. 1228690-19-4

AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release.

AM966

AM966

🥰Excellent
Purity: 99.79%
Catalog No. T4278Cas No. 1228690-19-4
AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$33In StockIn Stock
10 mg$53In StockIn Stock
25 mg$98In StockIn Stock
50 mg$167In StockIn Stock
100 mg$268In StockIn Stock
200 mg$386In StockIn Stock
1 mL x 10 mM (in DMSO)$36In StockIn 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:99.79%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release.
Targets&IC50
LPA1:IC50=17 nM
In vitro
Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by either amitriptyline or mianserin. LPA-induced ERK1/2 activation is completely blocked by AM966 (100 nM), which selectively antagonizes LPA1 over LPA2-5, with an IC50 value of 3.8±0.4 nM. AM966 inhibits LPA1-mediated chemotaxis of human A2058 melanoma cells (IC50=138±43 nM), IMR-90 human lung fibroblasts (IC50=182±86 nM) and CHO mLPA1 cells (IC50=469±54 nM).
In vivo
In a 3-day bleomycin model, AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation.
Cell Research
AM966 (Chem Scene, Monmouth Junction, NJ, USA) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.5%) before use.CHO-K1 cells are grown to 80% confluency in 12-well plates, serum-starved for 24 h and incubated in serum-free medium with AM966. After 21 h, [3H]thymidine (0.5 μCi/well) is added and the incubation is continued for 3 h. The medium is then removed, and the cells are placed on ice and washed twice with 1 mL of ice-cold PBS containing 5% trichloroacetic acid. Cells are solubilized and [3H]thymidine incorporation is determined by liquid scintillation counting. Assays are performed in triplicate.
Animal Research
In fasted mice, received AM966 (10 mg/kg), which is prepared in water, by oral gavage.
Chemical Properties
Molecular Weight490.93
FormulaC27H23ClN2O5
Cas No.1228690-19-4
SmilesC[C@@H](OC(=O)Nc1c(C)noc1-c1ccc(cc1)-c1ccc(CC(O)=O)cc1)c1ccccc1Cl
Relative Density.1.330 g/cm3 at 20℃
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: 45 mg/mL (91.66 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 2 mg/mL (4.07 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0370 mL10.1848 mL20.3695 mL101.8475 mL
5 mM0.4074 mL2.0370 mL4.0739 mL20.3695 mL
10 mM0.2037 mL1.0185 mL2.0370 mL10.1848 mL
20 mM0.1018 mL0.5092 mL1.0185 mL5.0924 mL
50 mM0.0407 mL0.2037 mL0.4074 mL2.0370 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

You can also refer to dose conversion for different animals. More Dose Conversion

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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