EL244 | Autotaxin inhibitor / PPARγ agonist | Probechem Biochemicals

Chemical Structure : EL244

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EL244 (EL-244)

货号: PC-26686Not For Human Use, Lab Use Only.

EL244 (EL-244) is a first-in-class, dual acting autotaxin inhibitor and PPARγ agonist with IC50 of 0.05 uM for autotaxin (ATX) and EC50 of 1.3 uM for PPARγ.

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生物&药学活性

EL244 (EL-244) is a first-in-class, dual acting autotaxin inhibitor and PPARγ agonist with IC50 of 0.05 uM for autotaxin (ATX) and EC50 of 1.3 uM for PPARγ.
EL244 activates PPARγ selectively over PPARα and PPAR δ, binds to the PPARγ LBD with ITC KD of 1.3 uM.
EL244 is a type IV ATX inhibitor, binds to the hydrophobic pocket and the allosteric tunnel of ATX.
EL244 differentiates 3T3-L1 fibroblasts to adipocytes in the presence of insulin, induces the expression of several PPARγ target genes, such as adiponectin (Adipoq), fatty acid binding protein 4 (Fabp4), and CD36, as well as PPARγ itself.
EL244 attenuates bleomycin (BLM)-induced pulmonary fibrosis and restores respiratory functions alleviates pulmonary fibrosis in vivo and prevents fibrosis in human fibrotic precision-cut lung slices (PCLSs).

物理化学性质&存储条件

分子量	537.45
分子式	C25H26Cl2N2O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3,5-dichlorobenzyl 4-(2-(4-((2,4-dioxothiazolidin-5-yl)methyl)phenoxy)ethyl)piperidine-1-carboxylate

参考文献

1. Matralis AN, et al. Cell Rep Med. 2026 Apr 30:102778.

EL244 (EL-244)

生物&药学活性

物理化学性质&存储条件

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EL244 (EL-244)

生物&药学活性

物理化学性质&存储条件

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