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

WNK463 

Cat. No.: HY-100626 Purity: 99.07%
COA 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
Solution
10 mM * 1 mL in DMSO USD 184 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 184 In-stock
Solid
1 mg USD 100 In-stock
5 mg USD 180 In-stock
10 mg USD 260 In-stock
25 mg USD 480 In-stock
50 mg USD 760 In-stock
100 mg USD 1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Formula

C21H24F3N7O2
CAS No.
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 available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

Keywords:

WNK4632012607-27-9WNK 463WNK-463Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesInhibitorinhibitorinhibit

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