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S32826

Catalog No. T38488 CAS 1096770-84-1

S32826 is a highly potent inhibitor of autotaxin, exhibiting an IC50 value of 8.8 nM. It displays comparable inhibitory properties towards various autotaxin isoforms, including α, β, and γ. Furthermore, S32826 effectively inhibits the release of LPA from adipocytes.

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S32826, CAS 1096770-84-1

Pack Size	Availability	Price/USD
1 mg	35 days	$ 95.00
5 mg	35 days	$ 294.00
10 mg	35 days	$ 550.00

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Biological Description

Chemical Properties

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Description	S32826 is a highly potent inhibitor of autotaxin, exhibiting an IC50 value of 8.8 nM. It displays comparable inhibitory properties towards various autotaxin isoforms, including α, β, and γ. Furthermore, S32826 effectively inhibits the release of LPA from adipocytes.
Targets&IC50	ATX:8.8 nM (IC50)
In vitro	S32826, at concentrations ranging from 0.001 to 10 μM over a period of 10 days, dose-dependently reduces lyso-phosphatidic acid (LPA) secretion by 3T3-F442A adipocytes, with an IC 50 value of 90 nM and achieving a peak suppression of 80% at 500 nM[1]. Additionally, at a concentration of 1 μM for 24 hours, S32826 effectively blocks the Dexamethasone-induced surge in autotaxin (ATX) mRNA levels and lysophospholipase D (lysoPLD) activity in the conditioned media of HTM cells. It also prevents Dexamethasone-triggered phosphorylation of myosin light chain (MLC) and cofilin, as well as the mRNA overexpression of COL1A1 and COL4A1, alongside inhibiting the expression of α-SMA, fibronectin, and collagen-1 in HTM cells[2].
In vivo	Topical application of S32826 at concentrations ranging from 2 to 10 mM for 2 hours to 5 days leads to a dose- and time-dependent reduction in intraocular pressure (IOP) in rabbits[2]. A single intracameral injection of approximately 2 μM S32826 also decreases IOP in rabbits, maintaining the ocular hypotensive effect for over 48 hours[2]. However, when administered orally (p.o.), intraperitoneally (i.p.), subcutaneously (s.c.), or intravenously (i.v.) at a dose of 10 mg/kg, S32826 demonstrates poor in vivo stability and/or bioavailability[1].

Molecular Weight	397.496
Formula	C21H36NO4P
CAS No.	1096770-84-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Ferry G, et, al. S32826, a nanomolar inhibitor of autotaxin: discovery, synthesis and applications as a pharmacological tool. J Pharmacol Exp Ther. 2008 Dec;327(3):809-19. 2. Honjo M, et, al. Role of the Autotaxin-LPA Pathway in Dexamethasone-Induced Fibrotic Responses and Extracellular Matrix Production in Human Trabecular Meshwork Cells. Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):21-30. 3. Iyer P, et, al. Autotaxin-lysophosphatidic acid axis is a novel molecular target for lowering intraocular pressure. PLoS One. 2012;7(8):e42627.

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Keywords

S32826 1096770-84-1 S-32826 S 32826 inhibitor inhibit

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