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AM095 Potent LPA1 receptor antagonist

Catalog No.A3166
Size Price Stock Qty
10mM (in 1mL DMSO)
$115.00
In stock
5mg
$100.00
In stock
10mg
$140.00
In stock
50mg
$450.00
In stock
200mg
$950.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Harper K, R Lavoie R, et al. "The Hypoxic Tumor Microenvironment Promotes Invadopodia Formation and Metastasis through LPA1 Receptor and EGFR Cooperation." Mol Cancer Res. 2018 Jun 4. pii:molcanres.0649.2017. PMID:29866927
2. Szepanowski F, Szepanowski LP, et al. "Lysophosphatidic acid propagates post-injury Schwann cell dedifferentiation through LPA(1) signaling. Neurosci Lett." 2017 Oct 16;662:136-141. PMID:29051083

Quality Control

Chemical structure

AM095

Related Biological Data

AM095

Biological Activity

Description AM095 is a potent antagonist of LPA1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively.
Targets LPA1 receptor          
IC50 0.98 μM (recombinant human) 0.73 μM (recombinant mouse)          

Protocol

Cell experiment: [1]

Cell lines

MDA-MB-231 cells and SK-OV3 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

500 nM, 5 min

Applications

Cells were pretreated with AM-095 or vehicle for 5 min and then treated with 10 μM of LPE or LPA. AM-095 (500 nM) completely inhibited LPA-induced [Ca2+]i responses in both cell lines and LPE-induced [Ca2+]i responses in MDA-MB-231 cells. AM-095 (500 nM) did not affect LPE-induced [Ca2+] i responses in SK-OV3 cells.

Animal experiment : [2]

Animal models

Female CD-1 mice

Dosage form

Oral administration, 1–30 mg/kg

Applications

Mice received AM095 in a volume of 10 ml/kg 2 h before the intravenous LPA (300 μg/mouse) challenge. LPA stimulated histamine release in a dose-dependent manner, resulting in a nearly 14-fold stimulation at the highest concentration tested. AM095 dose-dependently inhibited histamine release with an ED50 of 8.3 mg/kg and a maximal reduction of 80% at a dose of 30 mg/kg. By plotting the percentage inhibition of histamine release versus AM095 plasma concentrations for each individual animal and assuming a maximum response of 80% we generated an EC50 of ~ 1.5 μM.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Park S J, Lee K P, Im D S. Action and Signaling of Lysophosphatidylethanolamine in MDA-MB-231 Breast Cancer Cells. Biomolecules & therapeutics, 2014, 22(2): 129.

[2] Swaney J S, Chapman C, Correa L D, 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.

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Chemical Properties

Cas No. 1345614-59-6 SDF Download SDF
Synonyms AM 095;AM-095
Chemical Name sodium;2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetate
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-].[Na+]
Formula C27H23N2NaO5 M.Wt 478.47
Solubility >23.9mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively [1].

In vitro, AM095 has shown to inhibit LPA1-induced chemotaxis of both mouse LPA1/CHO cells and human A2058 melanoma cells with IC50 values of 0.78 μM and 0.23μM [1].

In vivo, AM095 could dose-dependently block LPA-induced histamine release with an ED50 value of 8.3 mg/kg in mice. Additionally, AM095 has been revealed to remarkably reduce the BALF collagen and protein with an ED50 value of 10 mg/kg in lungs. AM095 has also shown to decrease both macrophage and lymphocyte infiltration induced by bleomycin in mice [1].

References:
[1] Swaney JS1, Chapman C, Correa LD, Stebbins KJ, Broadhead AR, Bain G, Santini AM, Darlington J, King CD, Baccei CS, Lee C, Parr TA, Roppe JR, Seiders TJ, Ziff J, Prasit P, Hutchinson JH, Evans JF, Lorrain DS. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700.