2123489-30-3

Usage

Uses

Used in Pharmaceutical Industry:
(5-chloro-2-(2-(methylamino)thiazol-4-yl)-pyridin-4-yl)(4-(4-chlorobenzyl)piperazin-1-yl)methanone is used as a potential active pharmaceutical ingredient for the development of new drugs, leveraging its complex structure and the presence of functional groups that are commonly associated with biological activity.
Used in Medicinal Chemistry Research:
(5-chloro-2-(2-(methylamino)thiazol-4-yl)-pyridin-4-yl)(4-(4-chlorobenzyl)piperazin-1-yl)methanone serves as a subject of study in medicinal chemistry research, where its properties, interactions with biological targets, and potential therapeutic effects are investigated to understand its full scope of applications and to explore its use in the treatment of various diseases.

Upstream product

• 97674-02-7 tributyl(1-ethoxyvinyl)stannane 
• 598-52-7 1-(methyl)-thiourea 
• 23145-88-2 1-[(4-chlorophenyl)methyl]piperazine 
• 88912-26-9 2,5-dichloro-4-pyridinecarboxylic acid 

Relevant academic research and scientific papers

Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models

The observed structure-activity relationship of three distinct ATP noncompetitive With-No-Lysine (WNK) kinase inhibitor series, together with a crystal structure of a previously disclosed allosteric inhibitor bound to WNK1, led to an overlay hypothesis defining core and side-chain relationships across the different series. This in turn enabled an efficient optimization through scaffold morphing, resulting in compounds with a good balance of selectivity, cellular potency, and pharmacokinetic profile, which were suitable for in vivo proof-of-concept studies. When dosed orally, the optimized compound reduced blood pressure in mice overexpressing human WNK1, and induced diuresis, natriuresis and kaliuresis in spontaneously hypertensive rats (SHR), confirming that this mechanism of inhibition of WNK kinase activity is effective at regulating cardiovascular homeostasis.