Recommanded Product: 4637-24-5In 2019 ,《Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors》 appeared in Journal of Medicinal Chemistry. The author of the article were 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. The article conveys some information:
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).N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5Recommanded Product: 4637-24-5) was used in this study.
N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Recommanded Product: 4637-24-5
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