2012607-27-9

Basic information

• Product Name: WNK463
• Synonyms: WNK463
• CAS NO: 2012607-27-9
• Molecular Formula: C21H24F3N7O2
• Molecular Weight: 463.4561696
• Mol File: 2012607-27-9.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Density: 1.43±0.1 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• PKA: 15.18±0.46(Predicted)
• CAS DataBase Reference: WNK463(CAS DataBase Reference)
• NIST Chemistry Reference: WNK463(2012607-27-9)
• EPA Substance Registry System: WNK463(2012607-27-9)

Safety Data

• Hazardous Substances Data: 2012607-27-9(Hazardous Substances Data)

Usage

Description

WNK463 is a pan-WNK kinase inhibitor that targets WNK1, WNK2, WNK3, and WNK4 kinases. It has been observed to influence blood pressure, heart rate, and the regulation of body fluid and electrolyte homeostasis in rodent models of hypertension.

Uses

Used in Pharmaceutical Industry:
WNK463 is used as a therapeutic agent for the treatment of hypertension. Its ability to target multiple WNK kinases allows it to modulate blood pressure and heart rate, as well as maintain the balance of body fluids and electrolytes.
Used in Research Applications:
In the field of medical research, WNK463 serves as a valuable tool for studying the roles of WNK kinases in various physiological processes. By inhibiting these kinases, researchers can gain insights into their functions and potential implications in hypertension and other related conditions.
Used in Drug Development:
WNK463 is utilized in the development of new drugs targeting WNK kinases for the treatment of hypertension and other related disorders. Its pan-WNK kinase inhibitory activity makes it a promising candidate for the creation of novel therapeutics that can effectively manage these conditions.

Biochem/physiol Actions

WNK463 is a high-affinity, ATP-competitive inhibitor against with-No-Lysine (K) kinases (hWNK1/3/4 IC50 = 5/6/9 nM with MBP & 1 μM ATP, hWNK2 IC50 = 1 nM with MBP & 2 μM ATP, hWNK1 IC50 = 41 nM with OSR1 & 0.5 μM ATP; hWNK1/4 KD = 3.71/3.84 by SPR), exhibiting weak affinity against only two other human kinases among a panel of 442. WNK463 downregulates the overexpressed OSR1 phosphorylation level in HEK293 cells (IC50 = 106 nM; 1 hr) and displays in vivo efficacy in rodent hypertension models (1-10 mg/kg in rats p.o., 10 mg/kg in hWNK1 transgenic mice p.o.) with good orally availability (F = 100%/mice & 74%/rats post 1.5 mg/kg p.o.).