Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WNK463 is a pan-WNK-kinase inhibitor. It effectively inhibits the in vitro kinase activity of all four WNK family members (WNK1/2/3/4).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 72.00 | |
5 mg | In stock | $ 146.00 | |
10 mg | In stock | $ 213.00 | |
25 mg | In stock | $ 362.00 | |
50 mg | In stock | $ 538.00 | |
100 mg | In stock | $ 777.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 148.00 |
Description | WNK463 is a pan-WNK-kinase inhibitor. It effectively inhibits the in vitro kinase activity of all four WNK family members (WNK1/2/3/4). |
Targets&IC50 | WNK4:9 nM, WNK1:5nM, WNK3:6nM, WNK2:1nM |
In vitro | WNK463 potently inhibited the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4). WNK463 also inhibited WNK1-catalyzed phosphorylation of the native WNK substrate, oxidative stress response 1 (OSR1) in a biochemical assay and in human embryonic kidney 293 (HEK293) cells that express exogenous OSR1 and that are activated by sorbitol-mediated osmotic stress[1]. |
In vivo | In rodent models of hypertension, WNK463 affects blood pressure and body fluid and electrolyte homeostasis. WNK463 is orally bioavailable in C57BL/6 mice (100%) and Sprague Dawley rats (74%), with a half-life of 3.6 and 2.1 h, respectively. In spontaneously hypertensive rats (SHRs), WNK463 administered orally (p.o.) at 1, 3, or 10 mg per kg body weight (mg/kg) p.o. achieved maximum plasma concentration (Cmax) values of 88, 441, and 1,170 nM, respectively. These exposures produced dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. Moreover, WNK463 produced significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates. Orally administered WNK463 also significantly decreased blood pressure in these hypertensive mice. WNK463 elicited in vivo cardiovascular and renal effects through WNK kinase inhibition[1]. |
Molecular Weight | 463.46 |
Formula | C21H24F3N7O2 |
CAS No. | 2012607-27-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 85 mg/mL (183.4 mM)
DMSO: 85 mg/mL (183.4 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
WNK463 2012607-27-9 Cell Cycle/Checkpoint Metabolism Serine/threonin kinase Ser/Thr Protease inhibit Serine proteases Inhibitor Serine endopeptidases Threonine proteases WNK-463 WNK 463 inhibitor