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MedChemExpress - Model ERG240 - ...

MedChemExpress - Model ERG240 - 1415683-79-2

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].

ERG240

MCE China：ERG240

Brand：MedChemExpress (MCE)

Cat. No.HY-W193545A

CAS：1415683-79-2

Purity：98.0%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：ERG240 (20 µM, 3 hours) significantly reduces Irg1 mRNA and protein levels, along with itaconate production, in human monocyte-derived macrophages[2]. ERG240 (5 µM and 10 µM, 24 hours) significantly inhibits migration in bone marrow-derived macrophages (BMDMs)[2].

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].

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. [Content Brief]

[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.

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。