AM095 (Free Acid) - CAS 1228690-36-5
Catalog number: 1228690-36-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C27H24N2O5
Molecular Weight:
456.49
COA:
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Targets:
LPL Receptor
Description:
AM095, an effective LPA1 receptor antagonist, has been found to decrease dermal fibrosis caused by attenuates bleomycin. IC50: 0.98 uM and 0.73 uM for human and mouse LPA1 respectively.
Purity:
98%
Appearance:
Powder
Synonyms:
AM095 (free acid); CHEMBL2182052; AM095; AM-095 (free base); AM 095 (parent compound)
Solubility:
DMSO: ≥ 67.3 mg/mL
Storage:
-20ºC Freeze
MSDS:
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Application:
AM095 is an effective LPA1 receptor antagonist that has been found to decrease dermal fibrosis caused by attenuates bleomycin.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
LNDDRUPAICPXIN-GOSISDBHSA-N
InChI:
InChI=1S/C27H24N2O5/c1-17-25(28-27(32)33-18(2)20-6-4-3-5-7-20)26(34-29-17)23-14-12-22(13-15-23)21-10-8-19(9-11-21)16-24(30)31/h3-15,18H,16H2,1-2H3,(H,28,32)(H,30,31)/t18-/m1/s1
Canonical SMILES:
CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)CC(=O)O
1.Intercellular Lipid Mediators and GPCR Drug Discovery.
Im DS Biomol Ther (Seoul). 2013 Nov;21(6):411-22. doi: 10.4062/biomolther.2013.080.
G-protein-coupled receptors (GPCR) are the largest superfamily of receptors responsible for signaling between cells and tissues, and because they play important physiological roles in homeostasis, they are major drug targets. New technologies have been developed for the identification of new ligands, new GPCR functions, and for drug discovery purposes. In particular, intercellular lipid mediators, such as, lysophosphatidic acid and sphingosine 1-phosphate have attracted much attention for drug discovery and this has resulted in the development of fingolimod (FTY-720) and AM095. The discovery of new intercellular lipid mediators and their GPCRs are discussed from the perspective of drug development. Lipid GPCRs for lysophospholipids, including lysophosphatidylserine, lysophosphatidylinositol, lysophosphatidylcholine, free fatty acids, fatty acid derivatives, and other lipid mediators are reviewed.
2.Lysophosphatidic acid propagates post-injury Schwann cell dedifferentiation through LPA
Szepanowski F;Szepanowski LP;Mausberg AK;Kleinschnitz C;Kieseier BC;Stettner M Neurosci Lett. 2018 Jan 1;662:136-141. doi: 10.1016/j.neulet.2017.10.023. Epub 2017 Oct 16.
Lysophosphatidic acid (LPA) is a pleiotropic signaling lipid that acts as ligand for at least six specific G-protein coupled receptors. Schwann cells (SC) are known to mainly express the LPA;1; receptor subtype. An emerging body of evidence has linked LPA with injury-induced peripheral nerve demyelination as well as neuropathic pain. However, the molecular mechanisms underlying its demyelinating effect have not been conclusively elucidated. We aimed to decipher the demyelinating effect in vitro as well as in vivo by studying markers of SC differentiation and dedifferentiation: Myelinated dorsal root ganglia (DRG) cultures were treated either with LPA, LPA plus AM095 (LPA;1; antagonist) or vehicle. Myelin content was subsequently investigated by Sudan Black staining and immunocytochemistry. In vivo, we performed sciatic nerve crush in C57BL/6 mice treated with AM095 at 10mg/kg. In DRG cultures, LPA caused a significant reduction of myelin as demonstrated by both Sudan Black staining and immunocytochemical analysis of myelin basic protein. Demyelination was paralleled by an upregulation of TNF-alpha as well as downregulation of Sox10, a marker for SC differentiation. LPA mediated effects were largely blocked by the addition of the LPA;1; receptor antagonist AM095.
3.Action and Signaling of Lysophosphatidylethanolamine in MDA-MB-231 Breast Cancer Cells.
Park SJ;Lee KP;Im DS Biomol Ther (Seoul). 2014 Feb;22(2):129-35. doi: 10.4062/biomolther.2013.110.
Previously, we reported that lysophosphatidylethanolamine (LPE), a lyso-type metabolite of phosphatidylethanolamine, can increase intracellular Ca(2+) ([Ca(2+)]i) via type 1 lysophosphatidic acid (LPA) receptor (LPA1) and CD97, an adhesion G-protein-coupled receptor (GPCR), in MDA-MB-231 breast cancer cells. Furthermore, LPE signaling was suggested as like LPA1/CD97-Gi/o proteins-phospholipase C-IP3-Ca(2+) increase in these cells. In the present study, we further investigated actions of LPE not only in the [Ca(2+)]i increasing effect but also in cell proliferation and migration in MDA-MB-231 breast cancer cells. We utilized chemically different LPEs and a specific inhibitor of LPA1, AM-095 in comparison with responses in SK-OV3 ovarian cancer cells. It was found that LPE-induced Ca(2+) response in MDA-MB-231 cells was evoked in a different manner to that in SK-OV3 cells in terms of structural requirements. AM-095 inhibited LPE-induced Ca(2+) response and cell proliferation in MDA-MB-231 cells, but not in SK-OV3 cells, supporting LPA1 involvement only in MDA-MB-231 cells. LPA had significant effects on cell proliferation and migration in MDA-MB-231 cells, whereas LPE had less or no significant effect.
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CAS 1228690-36-5 AM095 (Free Acid)

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