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AM095 free acid

Catalog No. T10293 CAS 1228690-36-5

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

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AM095 free acid, CAS 1228690-36-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 67.00
5 mg	In stock	$ 91.00
10 mg	In stock	$ 139.00
50 mg	In stock	$ 398.00
100 mg	In stock	$ 635.00
200 mg	In stock	$ 947.00
500 mg	In stock	$ 1,697.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 99.9%

Biological Description

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Storage & Solubility Information

Description	AM095 (free acid) is a potent LPA1 receptor antagonist (IC50s: 0.98 and 0.73 μM for recombinant human or mouse LPA1).
Targets&IC50	human LPA1:0.98 μM , mouse LPA1:0.73 μM
In vitro	In vitro, AM095 was a potent LPA receptor antagonist because it inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA with IC values of 0.98 and 0.73 μM, respectively, and exhibited no LPA agonism.?In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA (IC = 778 nM) and human A2058 melanoma cells (IC = 233 nM)[3].
In vivo	In vivo, AM095: 1) had high oral bioavailability and a moderate half-life and was well tolerated at the doses tested in rats and dogs after oral and intravenous dosing, 2) dose-dependently reduced LPA-stimulated histamine release, 3) attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and 4) decreased kidney fibrosis in a mouse unilateral ureteral obstruction model[3].

Molecular Weight	456.49
Formula	C27H24N2O5
CAS No.	1228690-36-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 67.3 mg/mL (147.43 mM), Need ultrasonic and warming

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. 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. 2. 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. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

Neuronal Signaling Compound Library NO PAINS Compound Library Bioactive Compound Library ReFRAME Related Library GPCR Compound Library Inhibitor Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

GLPG2938 ONO-7300243 GSK2018682 Ki16198 SLF1081851 Ki16425 PF-543 CYM-5541

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AM095 free acid 1228690-36-5 GPCR/G Protein LPL Receptor LPA Receptor AM 095 Inhibitor AM-095 free acid inhibit AM095 Lysophospholipid Receptor AM-095 inhibitor

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