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Chemical Structure| 1228690-36-5 Chemical Structure| 1228690-36-5

Structure of AM095 free acid
CAS No.: 1228690-36-5

Chemical Structure| 1228690-36-5

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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.

Synonyms: AM095

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Product Details of AM095 free acid

CAS No. :1228690-36-5
Formula : C27H24N2O5
M.W : 456.49
SMILES Code : 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
Synonyms :
AM095
MDL No. :MFCD22665734
InChI Key :LNDDRUPAICPXIN-GOSISDBHSA-N
Pubchem ID :46213949

Safety of AM095 free acid

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of AM095 free acid

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human brain microvascular endothelial cells (HBMEC) 10 μM LPA increased permeability in HBMEC. PMC9024554
CHO cells 0.98 μM, 0.73 μM Inhibited LPA-induced calcium flux PMC10631474
HK-2 cells 10 μM 48 h AM095 inhibits LPA-induced expression of EMT markers and fibrotic factors PMC9500642
E11 cells 10 µm 4.5 h Assess pyroptosis. LPA significantly increased the number of pyroptotic cells, while AM095 significantly suppressed this increase. PMC10298531
E11 cells 10 µM 3 or 6 h Measure protein levels of NEK7, NLRP3, ASC, cleaved-caspase-1, N-GSDMD, and IL-1β. LPA significantly increased the expression of these factors, while AM095 significantly suppressed LPA-induced expression. PMC10298531
Mouse primary microglia 2 μM 30 min pretreatment followed by 24 h Suppressing LPA1 activity reduced mRNA expression levels of proinflammatory cytokines (TNF-α, IL-6, IL-1β) in LPS-stimulated microglia PMC6701099
Mouse brain microvascular endothelial cells (MBMEC) 10 μM 6 h AM095 significantly attenuated the LPA-induced changes in endothelial permeability and junctional proteins. PMC9024554
GLUTag L-cells 2.5 μM 2.5 h To test whether LPA inhibits GLP-1 secretion through LPAR1/3 signaling. Results showed LPA significantly inhibited GLP-1 secretion, and this inhibition was reversed by the LPAR1/3 antagonist Ki16425 PMC9025735
Primary hippocampal neurons 300 nM 45 min OX-A induces 2-AG biosynthesis via OX-1R, which is then converted to 2-AGP, leading to increased pT231-Tau phosphorylation PMC9710385

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice STZ-induced diabetic mice Oral 30 mg/kg Once daily for 8 weeks Evaluate the effect of AM095 on podocyte loss and death in the kidneys of STZ-induced diabetic mice. AM095 significantly inhibited podocyte loss and death. PMC10298531
ICR mice Transient middle cerebral artery occlusion (tMCAO) model Oral gavage 30 mg/kg Single dose immediately after reperfusion, assessed at 1 or 3 days post-tMCAO AM095 significantly attenuated tMCAO-induced brain infarction and neurological deficits, and suppressed microglial activation, proliferation, and proinflammatory responses PMC6701099
Lewis rats Experimental autoimmune neuritis (EAN) Oral gavage 10 mg/kg Once daily from 10 to 28 days post-immunization To evaluate the effect of AM095 on clinical scores and remyelination in EAN. Results showed significant improvement in clinical scores, particularly during the remission phase, and an increase in the number of large-caliber myelinated axons. PMC8680309
C57BL/6J mice Ischemia-reperfusion model Intraperitoneal injection 30 mg/kg Single dose The ATX inhibitor PF8380 significantly attenuated ATX activity and permeability in mouse brains. PMC9024554
Mice C57Bl/6J male mice Intraperitoneal injection 50 mg/kg Single injection, measured after 30 minutes To test whether LPA inhibits GLP-1 secretion in vivo. Results showed LPA caused an ~50% fall in circulating GLP-1, and this effect was prevented by LPAR1/3 antagonist Ki16425 PMC9025735

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL

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