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WNK463
🥰Excellent
Catalog No. T7017Cas No. 2012607-27-9
WNK463 is a pan-WNK-kinase inhibitor. It effectively inhibits the in vitro kinase activity of all four WNK family members (WNK1/2/3/4).
WNK463
🥰Excellent
Purity: 100%
Catalog No. T7017Cas No. 2012607-27-9
WNK463 is a pan-WNK-kinase inhibitor. It effectively inhibits the in vitro kinase activity of all four WNK family members (WNK1/2/3/4).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $72 | In Stock | |
| 5 mg | $146 | In Stock | |
| 10 mg | $213 | In Stock | |
| 25 mg | $362 | In Stock | |
| 50 mg | $538 | In Stock | |
| 100 mg | $777 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $148 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | WNK463 is a pan-WNK-kinase inhibitor. It effectively inhibits the in vitro kinase activity of all four WNK family members (WNK1/2/3/4). |
| Targets&IC50 | WNK4:9 nM, WNK1:5nM, WNK2:1nM, WNK3:6nM |
| In vitro | WNK463 potently inhibited the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4). WNK463 also inhibited WNK1-catalyzed phosphorylation of the native WNK substrate, oxidative stress response 1 (OSR1) in a biochemical assay and in human embryonic kidney 293 (HEK293) cells that express exogenous OSR1 and that are activated by sorbitol-mediated osmotic stress[1]. |
| In vivo | In rodent models of hypertension, WNK463 affects blood pressure and body fluid and electrolyte homeostasis. WNK463 is orally bioavailable in C57BL/6 mice (100%) and Sprague Dawley rats (74%), with a half-life of 3.6 and 2.1 h, respectively. In spontaneously hypertensive rats (SHRs), WNK463 administered orally (p.o.) at 1, 3, or 10 mg per kg body weight (mg/kg) p.o. achieved maximum plasma concentration (Cmax) values of 88, 441, and 1,170 nM, respectively. These exposures produced dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. Moreover, WNK463 produced significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates. Orally administered WNK463 also significantly decreased blood pressure in these hypertensive mice. WNK463 elicited in vivo cardiovascular and renal effects through WNK kinase inhibition[1]. |
| Molecular Weight | 463.46 |
| Formula | C21H24F3N7O2 |
| Cas No. | 2012607-27-9 |
| Smiles | CC(C)(C)NC(=O)c1cncn1C1CCN(CC1)c1ccc(cn1)-c1nnc(o1)C(F)(F)F |
| Relative Density. | 1.43 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 85 mg/mL (183.4 mM) DMSO: 85 mg/mL (183.4 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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