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ChemicalBook--->CAS DataBase List--->2012607-27-9

2012607-27-9

2012607-27-9 Structure

2012607-27-9 Structure
IdentificationBack Directory
[Name]

WNK463
[CAS]

2012607-27-9
[Synonyms]

WNK463
CS-2515
WNK 463;WNK-463
1H-Imidazole-5-carboxamide, N-(1,1-dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-
[Molecular Formula]

C21H24F3N7O2
[MDL Number]

MFCD30489744
[MOL File]

2012607-27-9.mol
[Molecular Weight]

463.46
Chemical PropertiesBack Directory
[density ]

1.43±0.1 g/cm3(Predicted)
[storage temp. ]

Sealed in dry,2-8°C
[solubility ]

DMSO : ≥ 30 mg/mL (64.73 mM)
[form ]

Solid
[pka]

15.18±0.46(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

WNK 463, is a pan-WNK kinase inhibitor, acting on WNK1, WNK2, WNK3, and WNK4 kinases. It has shown to affect blood pressure, heart rate, body fluid and electrolyte homeostasis in rodent models of hypertension.
[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.).
[storage]

Store at -20°C
Spectrum DetailBack Directory
[Spectrum Detail]

WNK463(2012607-27-9)1HNMR
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