S32826
S32826 is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes.
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- CAS. Nr.: 1096770-84-1
- Formel: C21H36NO4P
- Molecular Weight:397.49
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Autotaxin 8.8 nM (IC50) |
In Vitro
S32826 (0.001-10 μM; 10 days) dose-dependently inhibits the release of lyso-phosphatidic acid (LPA) by 3T3-F442A adipocytes with an IC50 of 90 nM and a maximal inhibition of 80% at 500 nM[1].
S32826 (1 μM; 24 h) inhibits Dexamethasone-induced increases in autotaxin (ATX) mRNA expression in HTM cells and lysoPLD activity in conditioned media. S32826 inhibits Dexamethasone-induced the phosphorylation of MLC and cofilin, mRNA upregulation of COL1A1 and COL4A1, and expression of α-SMA, fibronectin and collagen-1 in the HTM cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
S32826 (∼2 µM; single intracameral injection) reduces the IOP in rabbits, with the ocular hypotensive response lasting for more than 48 hrs[2].
S32826 (10 mg/kg; p.o., i.p., s.c., and i.v.) shows poor in vivo stability and/or bioavailability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1096770-84-1
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Molecular Weight 397.49
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Formel C21H36NO4P
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SMILES
O=C(NC1=CC=C(C=C1)CP(O)(O)=O)CCCCCCCCCCCCC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Large-size fat particle sorting
Large-size fat particle sorting is widely used to isolate cells up to 200 μm in diameter. Single-cell flow sorting will allow greater insight into adipocyte heterogeneity by identifying gene expression, protein composition, and metabolic signatures at the single-cell level.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
[3]. Iyer P, et, al. Autotaxin-lysophosphatidic acid axis is a novel molecular target for lowering intraocular pressure. PLoS One. 2012;7(8):e42627. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
S32826 Related Classifications
HY-103267A Related Classifications
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