1. GPCR/G Protein
  2. LPL Receptor
  3. AM966

AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).

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

AM966 Chemical Structure

AM966 Chemical Structure

CAS No. : 1228690-19-4

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 76 In-stock
Solution
10 mM * 1 mL in DMSO USD 76 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 110 In-stock
50 mg USD 340 In-stock
100 mg USD 540 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    AM966 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2016 Dec 30;291(53):27364-27370.  [Abstract]

    Effect of LPAR antagonists on ERK1/2 phosphorylation and FRS2 phosphorylation evoked by either amitriptyline (A) or LPA (B).

    AM966 purchased from MedChemExpress. Usage Cited in: J Pharmacol Exp Ther. 2016 Nov;359(2):340-353.  [Abstract]

    Concentration-dependent effects of LPA receptor antagonists on antidepressant- and LPA-induced ERK1/2 phosphorylation in C6 glioma cells. Cells are pre-incubated with either vehicle or the indicated concentrations of AM966 for 10 min and then exposed to either vehicle or 1 μM LPA (A), 15 μM Amitriptyline (C) or 5 μM Mianserin (E) for 10 min.

    AM966 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2015 Jun 15;95(4):311-23.  [Abstract]

    CHO-K1 cells express LPA1 receptors coupled to ERK1/2 phosphorylation. Inhibition of LPA-induced phospho-ERK1/2 by AM966. Cells are pre-incubated with either vehicle or the indicated concentrations of AM966 for 30 min and then treated with LPA (300 nM) for 15 min. Values are expressed as percent of p-ERK stimulation elicited by LPA in the absence of antagonist and are the mean ± SEM of three experiments.

    AM966 purchased from MedChemExpress. Usage Cited in: College of Pharmacy. Washington State University. 2015 May.

    Effects of LPAR antagonists on growth factor-induced phosphorylation of ERK in DU145 cells. Serum starved DU145 cells are incubated with 10 μM LPA, with or without either 100 nM AM966 or 10 μM Ki16425 for 10 minutes. Whole-cell extracts, equalized for protein, are immunoblotted for phospho-ERK (pERK) and for actin (loading control).

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).

    IC50 & Target

    LPA1[1]

    In Vitro

    AM966 is a potent, selective, orally bioavailable LPA1 receptor antagonist. 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)[1]. 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. Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by Mianserin[2].

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

    In Vivo

    AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation in a 3 day Bleomycin (HY-108345) model. AM966 inhibits lung fibrosis, maintains mouse body weight and decreases lung inflammation 14 days after Bleomycin lung injury. AM966 reduces vascular leakage, tissue injury and pro-fibrotic cytokine production in the 14 day Bleomycin study. AM966 demonstrates greater efficacy compared to Pirfenidone (HY-B0673) in the 14 day Bleomycin model. AM966 decreases mortality and fibrosis at late time points after Bleomycin injury[1].

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

    Molecular Weight

    490.93

    Formula

    C27H23ClN2O5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)CC1=CC=C(C2=CC=C(C3=C(NC(O[C@@H](C4=CC=CC=C4Cl)C)=O)C(C)=NO3)C=C2)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (203.70 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 2.0370 mL 10.1848 mL 20.3695 mL
    5 mM 0.4074 mL 2.0370 mL 4.0739 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)

    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 (5.09 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (20.37 mM); Suspended solution; Need ultrasonic

    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
    Cell Assay
    [2]

    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[2].

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

    Animal Administration
    [1]

    Mice[1]
    The oral exposure of AM966 is determined in fasted mice. Animals received AM966 (10 mg/kg) in vehicle (water) by oral gavage and are then killed by CO2 inhalation at 1, 2, 4, 8 and 24 h post dose (n=2 animals per time point for each test compound). Blood (approximately 300 µL) is collected via cardiac puncture into EDTA-containing tubes and centrifuged at 1450×g for 10 min. The plasma is removed and analysed for AM966 content by liquid chromatography-mass spectrometry (LCMS). Briefly, known amounts of AM966 are added to thawed mouse plasma to yield a concentration range from 0.8 to 4000 ng/mL. Mouse plasma samples are precipitated using acetonitrile (1:4, v:v) containing the internal standard buspirone. A 10 µL aliquot of the analyte mixture is injected using a Leap PAL autosampler. Analyses are performed using an Agilent Zorbax SB-C8 column (2.1×50 mm; 5 µm) linked to a Shimadzu LC-10AD VP with SCL-10A VP system controller. Tandem mass spectrometric detection is carried out on a PE Sciex API3200 in the positive ion mode (ESI) by multiple reaction monitoring. The calibration curves are constructed by plotting the peak-area ratio of analysed peaks against known concentrations. The lower limit of quantitation is 0.8 ng/mL. The data are subjected to linear regression analysis with 1/x2weighting.

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

    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, 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 2.0370 mL 10.1848 mL 20.3695 mL 50.9238 mL
    5 mM 0.4074 mL 2.0370 mL 4.0739 mL 10.1848 mL
    10 mM 0.2037 mL 1.0185 mL 2.0370 mL 5.0924 mL
    15 mM 0.1358 mL 0.6790 mL 1.3580 mL 3.3949 mL
    20 mM 0.1018 mL 0.5092 mL 1.0185 mL 2.5462 mL
    25 mM 0.0815 mL 0.4074 mL 0.8148 mL 2.0370 mL
    30 mM 0.0679 mL 0.3395 mL 0.6790 mL 1.6975 mL
    40 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2731 mL
    50 mM 0.0407 mL 0.2037 mL 0.4074 mL 1.0185 mL
    60 mM 0.0339 mL 0.1697 mL 0.3395 mL 0.8487 mL
    80 mM 0.0255 mL 0.1273 mL 0.2546 mL 0.6365 mL
    100 mM 0.0204 mL 0.1018 mL 0.2037 mL 0.5092 mL
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    AM966 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.

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    Cat. No.:
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