WNK463

SKU: orb1225751

Description

The first, potent, selective, and orally bioavailable pan With-No-Lysine (WNK) Kinase catalytic activity inhibitor with IC50 of 5/1/6/9 nM for WNK1/2/3/4, respectively; shows >50% inhibition against only 2 out of 442 human kinases at 10 uM; affects blood pressure and body fluid and electro-lyte homeostasis in rodent models of hypertension.

Key Properties

• CAS Number: 2012607-27-9
• MW: 463.4562
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₄F₃N₇O₂
• SMILES: O=C(C1=CN=CN1C2CCN(C3=NC=C(C4=NN=C(C(F)(F)F)O4)C=C3)CC2)NC(C)(C)C
• Target: WNK Kinase
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• In Vivo:
  Animal model: Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age). Dosage: 1 mg/kg, 3 mg/kg, or 10 mg/kg(Pharmacokinetic study). Administration: Oral administration; 4 hours. Result: Decreased in blood pressure and simultaneous increases in heart rate. WNK463 produced significant and dose-dependent increased in urine output as well as urinary sodium and potassium excretion rates.
• In Vitro:
  Western blot analysis. Cell line: Human tissue-engineered corneas (hTECs). Concentration: 50 nM, 1 μΜ, 10 μΜ. Incubation time: 6 days. Result: Reduced phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WNK-463 | WNK 463

Quick Database Links

Gene Symbol

WNK Kinase