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AM095 Inhibitor – Free Acid

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5752679

AM095 (free acid) is a potent LPA1 receptor antagonist (IC50s: 0.98 and 0.73uM for recombinant human or mouse LPA1). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
AM095 free acid, Inhibitor
Full Product Name
AM095 free acid
Product Gene Name
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
456.49
Solubility
DMSO: 67.3mg/mL (147.43mM) Need ultrasonic and warming
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C27H24N2O5
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
CAS Number
1228690-36-5
Target & IC50
human LPA1: ic50 0.98uM
mouse LPA1: ic50 0.73uM
In Vitro
Pharmacological antagonism of LPA1 with AM095 significantly attenuates bleomycin-induced dermal fibrosis [1]. AM095 dose-dependently reduces LPA-stimulated histamine release. AM095 attenuates bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchoalveolar lavage fluid. 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 decreases kidney fibrosis in a mouse unilateral ureteral obstruction model [3].

Product Categories/Family for AM095, inhibitor

Product References and Citations for AM095, inhibitor

Castelino FV, et al. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma. Arthritis Rheum. 2011 May;63(5):1405-15.
Castelino FV, et al. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma. Arthritis Rheum. 2011 May;63(5):1405-15.
Ruisanchez E, et al. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J. 2014 Feb;28(2):880-90.
Ruisanchez E, et al. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J. 2014 Feb;28(2):880-90.
Swaney, J. S., et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Journal of Pharmacology and Experimental Therapeutics (2011), 336(3), 693-700.
Swaney, J. S., et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Journal of Pharmacology and Experimental Therapeutics (2011), 336(3), 693-700.

Other Notes

Small volumes of AM095, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for AM095 purchase

MBS5752679 is an inhibitor targeting AM095. Also known as AM095 free acid.
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