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ERG240

Chemical Structure : ERG240

CAS No.: 1415683-79-2

ERG240 (ERG-240)

货号: PC-26613Not For Human Use, Lab Use Only.

ERG240 (ERG-240) is a potent, selective, orally active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor, inhibits recombinant BCAT1 with an IC50 of 0.1-1 nM, with no inhibition on BCAT2.

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10 mg ¥780 In stock
25 mg ¥1280 In stock
50 mg ¥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ERG240 (ERG-240) is a potent, selective, orally active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor, inhibits recombinant BCAT1 with an IC50 of 0.1-1 nM, with no inhibition on BCAT2.
ERG240 (3 h, 20 mM) treatment induced reduction in IRG1 mRNA levels but not HIF1A and IL1B in LPS-stimulated cells, resulted in decreased itaconate levels.
ERG240 showed comparable inhibitory effect on IRG1 expression in TNF-stimulated human macrophages and long-term exposure (24 h) to LPS and ERG240 resulted in reduced IL-1β levels. ERG240 significantly reduced TNF and NOS2 but not IL6 and PTGS2 expression levels in human macrophages.
ERG240 blocked itaconate production in vivo and polarizes peritoneal macrophages.
ERG240 reduced the severity of crescentic glomerulonephritis in rats and CIA in mice.

物理化学性质&存储条件

分子量 166.15
分子式 C7H11NaO3
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

Sodium 4-methyl-5-oxohexanoate

参考文献

1. Papathanassiu AE, et al. Nat Commun. 2017 Jul 12;8:16040.

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