1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. WNK463

WNK463 

Cat. No.: HY-100626 Purity: 99.55%
Handling Instructions

WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively.

For research use only. We do not sell to patients.

WNK463 Chemical Structure

WNK463 Chemical Structure

CAS No. : 2012607-27-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 196 In-stock
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively[1].

IC50 & Target

IC50: 5 nM (WNK1), 1 nM (WNK2), 6 nM (WNK3), and 9 nM (WNK4)[1]

In Vitro

WNK463 (50 nM, 1 μΜ, 10 μΜ; 6 days; Human tissue-engineered corneas (hTECs)) treatment reduces phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs.

Western Blot Analysis[2]

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.
In Vivo

WNK463 (1-10 mg/kg; oral administration; 4 hours; Spontaneously hypertensive Sprague Dawley rats) treatment produces dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. WNK463 produces significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates.
WNK463 is orally bioavailable in Sprague Dawley rats with a half-life of 2.1 hours[1].

Animal Model: Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age) [1]
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.
Molecular Weight

463.46

Formula

C₂₁H₂₄F₃N₇O₂

CAS No.

2012607-27-9

SMILES

FC(F)(F)C1=NN=C(O1)C2=CN=C(N3CCC(N4C=NC=C4C(NC(C)(C)C)=O)CC3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (64.73 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1577 mL 10.7884 mL 21.5768 mL
5 mM 0.4315 mL 2.1577 mL 4.3154 mL
10 mM 0.2158 mL 1.0788 mL 2.1577 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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WNK463
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HY-100626
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