Home GPCR & G Protein LPA Receptor antagonist AM 095 For research use only.

AM 095

AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively.

AM 095 Chemical Structure

AM 095 Chemical Structure

CAS No. 1228690-36-5

Purity & Quality Control

AM 095 Related Products

Signaling Pathway

LPA Receptor Signaling Pathways

LPA Receptor Signaling Pathway

Biological Activity

Description AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively.
Targets
LPA1 receptor [1]
In vitro
In vitro

AM095 is a potent LPA1 receptor antagonist because it inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively, and exhibited no LPA1 agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM)[1].
In Vivo
In vivo

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. It dose-dependently reduceS LPA-stimulated histamine release, attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and decreases kidney fibrosis in a mouse unilateral ureteral obstruction model. Despite its antifibrotic activity, AM095 has no effect on normal wound healing after incisional and excisional wounding in rats[1].
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 2 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 456.49 Formula

C27H24N2O5
CAS No. 1228690-36-5 SDF --
Smiles CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2)C3=CC=C(C=C3)C4=CC=C(C=C4)CC(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (199.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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