Organobromine compounds, also called organobromides, are organic compounds that contain carbon bonded to bromine. 70-23-5, formula is C5H7BrO3, The most pervasive is the naturally produced bromomethane. COA of Formula: C5H7BrO3
Rai, Ganesha;Urban, Daniel J.;Mott, Bryan T.;Hu, Xin;Yang, Shyh-Ming;Benavides, Gloria A.;Johnson, Michelle S.;Squadrito, Giuseppe L.;Brimacombe, Kyle R.;Lee, Tobie D.;Cheff, Dorian M.;Zhu, Hu;Henderson, Mark J.;Pohida, Katherine;Sulikowski, Gary A.;Dranow, David M.;Kabir, Md;Shah, Pranav;Padilha, Elias;Tao, Dingyin;Fang, Yuhong;Christov, Plamen P.;Kim, Kwangho;Jana, Somnath;Muttil, Pavan;Anderson, Tamara;Kunda, Nitesh K.;Hathaway, Helen J.;Kusewitt, Donna F.;Oshima, Nobu;Cherukuri, Murali;Davies, Douglas R.;Norenberg, Jeffrey P.;Sklar, Larry A.;Moore, William J.;Dang, Chi V.;Stott, Gordon M.;Neckers, Leonard;Flint, Andrew J.;Darley-Usmar, Victor M.;Simeonov, Anton;Waterson, Alex G.;Jadhav, Ajit;Hall, Matthew D.;Maloney, David J. research published 《 Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties》, the research content is summarized as follows. Lactate dehydrogenase (LDH) catalyzes the conversion of pyruvate to lactate, with concomitant oxidation of reduced NAD as the final step in the glycolytic pathway. Glycolysis plays an important role in the metabolic plasticity of cancer cells and has long been recognized as a potential therapeutic target. Thus, potent, selective inhibitors of LDH represent an attractive therapeutic approach. However, to date, pharmacol. agents have failed to achieve significant target engagement in vivo, possibly because the protein is present in cells at very high concentrations We report herein a lead optimization campaign focused on a pyrazole-based series of compounds, using structure-based design concepts, coupled with optimization of cellular potency, in vitro drug-target residence times, and in vivo PK properties, to identify first-in-class inhibitors that demonstrate LDH inhibition in vivo. The lead compounds, named NCATS-SM1440 (43)(I) and NCATS-SM1441 (52)(II), possess desirable attributes for further studying the effect of in vivo LDH inhibition.
COA of Formula: C5H7BrO3, Ethyl bromopyruvate molecular formula is C5H7BrO3 and its molecular weight is 195.01 g/mol. The purity is usually 95%.
Ethyl bromopyruvate is used in a synthesis of thioxothiazolidines from carbon disulfide and primary amines.
Ethyl bromopyruvate is a chemical inhibitor that inhibits the enzyme pyruvate dehydrogenase, which is responsible for the conversion of pyruvic acid to acetyl-CoA. This inhibition leads to a decrease in ATP levels and can cause metabolic disorders. Ethyl bromopyruvate is used as an anthelmintic drug and in asymmetric synthesis. It is also used in the synthesis of thiostrepton, an antibiotic that has been shown to have antimicrobial activity against Gram-positive bacteria, including Staphylococcus aureus and Streptococcus pneumoniae., 70-23-5.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary