| Identification | Back 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 Properties | Back 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) | [pka]
15.18±0.46(Predicted) |
| Hazard Information | Back 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 |
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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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