1. GPCR/G Protein
  2. LPL Receptor
  3. AM095 free acid

AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

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

AM095 free acid Chemical Structure

AM095 free acid Chemical Structure

CAS No. : 1228690-36-5

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 105 In-stock
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5 mg USD 95 In-stock
10 mg USD 150 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of AM095 free acid:

Top Publications Citing Use of Products

    AM095 free acid purchased from MedChemExpress. Usage Cited in: Biomol Ther (Seoul). 2014 Feb;22(2):129-35.  [Abstract]

    Efficacies of LPE- and LPA-induced Ca2+ responses as compared to digitonin in MDA-MB-231 and SK-OV3 cells are shown as histograms.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

    IC50 & Target

    IC50: 0.98 μM (human LPA1), 0.73 μM (mouse LPA1)

    In Vitro

    AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively[1]. AM095 reduces LPA-induced vasorelaxation by appr 90% at 10 μM as compared to vehicle control[2]. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM)[3].

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

    In Vivo

    Pharmacological antagonism of LPA1 with AM095 significantly attenuates bleomycin-induced dermal fibrosis[1]. AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. AM095 dose-dependently reduces LPA-stimulated histamine release. AM095 attenuates bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid. AM095 decreases kidney fibrosis in a mouse unilateral ureteral obstruction model[3].

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

    Molecular Weight

    456.49

    Formula

    C27H24N2O5

    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=C4)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 : 67.3 mg/mL (147.43 mM; Need ultrasonic and warming; 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 2.1906 mL 10.9531 mL 21.9063 mL
    5 mM 0.4381 mL 2.1906 mL 4.3813 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)

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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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    90% Corn Oil

      Solubility: ≥ 2.25 mg/mL (4.93 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.25 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 (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    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

    Purity: 98.24%

    References
    Kinase Assay
    [3]

    Assays are conducted using both hLPA1/CHO and mLPA1/CHO cells. A cell pellet of hLPA1/CHO or mLPA1/CHO cells is resuspended in appr 20 mL of ice-cold membrane buffer containing 10 mM HEPES, pH 7.4, 1 mM dithiothreitol, and protease inhibitors. Cells are sonicated, and the cell lysate is centrifuged at 2000 rpm for 10 min at 4°C. The supernatant is further centrifuged at 25,000 rpm for 70 min at 4°C. The membrane pellet is resuspended in 5 mL of ice-cold membrane buffer and homogenized using a Potter-Elvehjem tissue grinder. Final protein concentration is determined using the Bradford Protein Assay Kit. Known amounts of AM095 (diluted in dimethyl sulfoxide) or vehicle (dimethyl sulfoxide) are added to 25 to 40 μg of hLPA1/CHO or mLPA1/CHO membranes and 0.1 nM [35S]-GTPγS in buffer (50 mM HEPES, 0.1 mM NaCl, 10 mM MgCl2, 50 μg/mL saponin, pH 7.5) containing 0.2% fatty acid-free human serum albumin and 5 μM GDP. To test for LPA1 antagonist activity, the ability of AM095 to inhibit GTPγS binding stimulated by 900 nM LPA (18:1) is measured. Alternatively, to test for agonist effects, the ability of AM095 to stimulate GTPγS binding in the absence of LPA is measured. Reactions are incubated for 30 min at 30°C, before harvesting membranes onto glass filter binding plates and washing three times with cold buffer containing 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2 using a Brandel 96-tip cell harvester. Plates are dried and then cpm are evaluated by using a Packard TopCount NXT microplate scintillation counter.

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

    Animal Administration
    [3]

    Mice underwent UUO or sham surgery to the left kidney. In brief, a longitudinal, upper left incision is performed to expose the left kidney. The renal artery is located and a 6/0 silk thread is passed between the artery and the ureter. The thread is looped around the ureter and knotted three times insuring full ligation of ureter. The kidney is returned to abdomen, the abdominal muscle is sutured, and the skin is closed with staples. The contralateral (right) kidney served as an uninjured control. AM095 (30 mg/kg) or vehicle (water) is given 1 to 4 h before UUO and then b.i.d. thereafter by oral gavage. After 8 days, mice are euthanized using inhaled CO2, and the kidneys are harvested and cut in half for histopathological and biochemical analysis of fibrosis. To assess fibrosis, half of the kidney is fixed in 10% neutral buffered formalin and stained using Masson's trichrome. The other half of the kidney is frozen at −80°C for subsequent biochemical analysis of collagen content.

    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 2.1906 mL 10.9531 mL 21.9063 mL 54.7657 mL
    5 mM 0.4381 mL 2.1906 mL 4.3813 mL 10.9531 mL
    10 mM 0.2191 mL 1.0953 mL 2.1906 mL 5.4766 mL
    15 mM 0.1460 mL 0.7302 mL 1.4604 mL 3.6510 mL
    20 mM 0.1095 mL 0.5477 mL 1.0953 mL 2.7383 mL
    25 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1906 mL
    30 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8255 mL
    40 mM 0.0548 mL 0.2738 mL 0.5477 mL 1.3691 mL
    50 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
    60 mM 0.0365 mL 0.1826 mL 0.3651 mL 0.9128 mL
    80 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6846 mL
    100 mM 0.0219 mL 0.1095 mL 0.2191 mL 0.5477 mL
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    • 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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    Product Name:
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