Day: September 15, 2022

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Safety of 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Hou, Shaohua;Yang, Xiping;Tong, Yu;Yang, Yuejing;Chen, Quanwei;Wan, Boheng;Wei, Ran;Wang, Yuchen;Zhang, Yanmin;Kong, Bo;Huang, Jianhang;Chen, Yadong;Lu, Tao;Hu, Qinghua;Du, Ding research published 《 Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis》, the research content is summarized as follows. Apoptosis signal-regulating kinase 1 (ASK1), a member of the mitogen-activated protein kinase (MAPK) family, is implicated in many human diseases. Here, we describe the structural optimization of a hit compound and conduct further structure-activity relationship (SAR) studies that result in the development of the indole-2-carboxamide I. I displays potent anti-ASK1 kinase activity and stronger inhibitory effect on ASK1 in AP1-HEK293 cells than previously described ASK1 inhibitor GS-4997. Besides improved in vitro activity, I also exhibits an appropriate in vivo PK profile. In a dextran sulfate sodium (DSS)-induced mouse model of ulcerative colitis (UC), I shows significant anti-UC efficacy and markedly attenuates DSS-induced body weight loss, colonic shortening, elevation in disease activity index (DAI) and inflammatory cell infiltration in colon tissues. Mechanistically, I represses the phosphorylation of ASK1-p38/JNK signaling pathways and suppresses the overexpression of inflammatory cytokines. Together, these findings suggest that ASK1 inhibitors can potentially be used as a therapeutic strategy for UC.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Safety of 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Related Products of 2075-46-9.

Barzegar-Jalali, Mohammad;Rahimpour, Elaheh;Acree, William E. Jr.;Jouyban, Abolghasem research published 《 A global version of modified Wilson model for solubility prediction of drugs in methanol + water mixtures》, the research content is summarized as follows. The trained version of modified Wilson model is proposed employing solubility data of 41 drugs and/or drug-like compounds in methanol + water mixtures at various temperatures For covering the physicochem. properties of the solute to provide a QSPR model, the Abraham solvation parameters of solutes are combined with the modified Wilson model. The mean relative deviations for the correlated data are 32.5% and 27.1%, resp. for the modified Wilson model and its combined version with Abraham solvation parameters. Furthermore, an attempt is also made to correlate the solubility data with the modified Wilson model combined with van’t Hoff equation and the Abraham general solvation parameters to provide a full predictive model for drug solubility prediction in methanol + water mixtures at various temperatures

Related Products of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics