| Identification | Back Directory | [Name]
Hexanoic acid, 4-methyl-5-oxo-, sodium salt (1:1) | [CAS]
1415683-79-2 | [Synonyms]
ERG240
Hexanoic acid, 4-methyl-5-oxo-, sodium salt (1:1) | [Molecular Formula]
C7H13NaO3 | [MOL File]
1415683-79-2.mol | [Molecular Weight]
168.17 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, away from moisture and light | [solubility ]
DMSO : 100 mg/mL (601.87 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
ERG240 is an oral active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor. ERG240 can be used for the research of cancer, rheumatoid arthritis, and bone disease[1]. | [in vivo]
ERG240 (500 mg/kg, i.p., administered 30 min before and 8 h after LPS injection) significantly decreases pro-inflammatory response and increases anti-inflammatory transcriptomic features in LPS (HY-D1056)-induced acute inflammation C57BL/6 mouse model[2].
ERG240 (720 mg/kg and 1000 mg/kg, p.o., once daily for 3 weeks (720 mg/kg) and 4 weeks (1000 mg/kg)) significantly alleviates inflammation and joint destruction in the collagen-induced arthritis DBA/1 mouse model[2].
ERG240 (500 mg/kg, p.o., once daily for 10 days) significantly reduces the severity of inflammation and interstitial fibrosis in the NTN WKY rat model induced by nephrotoxic serum[2]. | Animal Model: | LPS (HY-D1056)-induced acute inflammation C57BL/6 mouse model[2] | | Dosage: | 500 mg/kg | | Administration: | Intraperitoneal injection (i.p.), administered 30 min before and 8 h after LPS injection | | Result: | Reduced Irg1 mRNA and protein levels along with itaconate production. |
| Animal Model: | Collagen (HY-NP102)-induced arthritis (CIA) DBA/1 mouse model[2] | | Dosage: | 720 and 1000 mg/kg | | Administration: | Oral gavage (p.o.), once daily for 3 weeks (720 mg/kg) and 4 weeks (1000 mg/kg) | | Result: | Significantly reduced inflammation, cartilage damage, pannus formation, and bone resorption in CIA model; decreased serum levels of pro-inflammatory markers TNF and RANKL. |
| Animal Model: | Nephrotoxic nephritis (NTN) WKY rat model induced by nephrotoxic serum (NTS) injection[2] | | Dosage: | 500 mg/kg | | Administration: | Oral gavage (p.o.), once daily for 10 days | | Result: | Reduced glomerular crescent formation, proteinuria, serum creatinine, and collagen type I levels. |
| [References]
[1] Papathanassiu, et al. Methods for treatment of cancer, inflammatory autoimmune disorders and bone diseases using branched-chain amino acid aminotransferase-1 (BCAT1) inhibitors. Patent. WO2012173987.
[2] Papathanassiu AE, et al. BCAT1 controls metabolic reprogramming in activated human macrophages and is associated with inflammatory diseases. Nat Commun. 2017 Jul 12;8:16040. DOI:10.1038/ncomms16040
[3] Papathanassiu A E, et al. Inhibition of BCAT1 suppresses the expression of pro-metastatic proteins and reduces cancer metastasis[J]. Cancer Research, 2014, 74(19_Supplement): 2683-2683. |
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