Category: 761446-44-0

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of 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. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Quality Control of 761446-44-0.

Yu, Mingfeng;Teo, Theodosia;Yang, Yuchao;Li, Manjun;Long, Yi;Philip, Stephen;Noll, Benjamin;Heinemann, Gary K.;Diab, Sarah;Eldi, Preethi;Mekonnen, Laychiluh;Anshabo, Abel T.;Rahaman, Muhammed H.;Milne, Robert;Hayball, John D.;Wang, Shudong research published 《 Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation》, the research content is summarized as follows. CDK8 regulates transcription either by phosphorylation of transcription factors or, as part of a four-subunit kinase module, through a reversible association of the kinase module with the Mediator complex, a highly conserved transcriptional coactivator. Deregulation of CDK8 has been found in various types of human cancer, while the role of CDK8 in suppressing anti-cancer response of natural killer cells is being understood. Currently, CDK8-targeting cancer drugs are highly sought-after. Herein authors detail the discovery of a series of novel pyridine-derived CDK8 inhibitors. Medicinal chem. optimization gave rise to I (AU1-100), a potent CDK8 inhibitor with oral bioavailability. The compound inhibited the proliferation of MV4-11 acute myeloid leukemia cells with the kinase activity of cellular CDK8 dampened. No systemic toxicol. was observed in the mice treated with I. These results warrant further pre-clin. studies of I as an anti-cancer agent.

Quality Control of 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%., 761446-44-0.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of 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. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Quality Control of 761446-44-0.

Adlington, Neil K.;Agnew, Lauren R.;Campbell, Andrew D.;Cox, Robert J.;Dobson, Andrew;Barrat, Cristina Fernandez;Gall, Malcolm A. Y.;Hicks, William;Howell, Gareth P.;Jawor-Baczynska, Anna;Miller-Potucka, Lucie;Pilling, Michael;Shepherd, Katy;Tassone, Ross;Taylor, Brian A.;Williams, Aled research published 《 Process Design and Optimization in the Pharmaceutical Industry: A Suzuki-Miyaura Procedure for the Synthesis of Savolitinib》, the research content is summarized as follows. A process for the Suzuki-Miyaura coupling reaction on multihundred kilogram scale as the final step in the preparation of the potential antitumor agent savolitinib I is developed. The optimization of catalyst and solvent for the process, the kinetics of the Suzuki-Miyaura coupling, the dependence of byproduct formation on solvent, temperature, and catalyst loading, and the development of procedures for the removal of palladium residues from the product and for the recrystallization of the unsolvated product as the desired form I are discussed. The requirements for and constraints on the large scale preparation of an active pharmaceutical ingredient are discussed.

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%., Quality Control of 761446-44-0

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

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