Himmelbauer, Martin K. team published research on Journal of Medicinal Chemistry in 2019 | 761446-44-0

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%., Formula: C10H17BN2O2

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Formula: C10H17BN2O2.

Himmelbauer, Martin K.;Xin, Zhili;Jones, J. Howard;Enyedy, Istvan;King, Kristopher;Marcotte, Douglas J.;Murugan, Paramasivam;Santoro, Joseph C.;Hesson, Thomas;Spilker, Kerri;Johnson, Joshua L.;Luzzio, Michael J.;Gilfillan, Rab;de Turiso, Felix Gonzalez-Lopez research published 《 Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors》, the research content is summarized as follows. Structural anal. of a known ASK1 inhibitor bound to its kinase domain led to the design and synthesis of the novel macrocyclic inhibitor I (cell IC50 = 1.2μM). The profile of this compound was optimized for CNS penetration following two independent strategies: a rational design approach leading to II and a parallel synthesis approach leading to III. Both analogs are potent ASK1 inhibitors in biochem. and cellular assays (II, cell IC50 = 95 nM; III, cell IC50 = 123 nM) and have moderate to low efflux ratio (ER) in an MDR1-MDCK assay (II, ER = 5.2; III, ER = 1.5). In vivo PK studies revealed that inhibitor II had moderate CNS penetration (Kp,uu = 0.17) and analog III had high CNS penetration (Kp,uu = 1.0).

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%., Formula: C10H17BN2O2

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