WNK463
- Product Name
- WNK463
- CAS No.
- 2012607-27-9
- Chemical Name
- WNK463
- Synonyms
- WNK463;CS-2515;WNK 463;WNK-463;Ser/Thr Protease,WNK 463,inhibit,WNK463,Serine proteases,Inhibitor,Serine endopeptidases,Threonine proteases,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]-
- CBNumber
- CB23145823
- Molecular Formula
- C21H24F3N7O2
- Formula Weight
- 463.46
- MOL File
- 2012607-27-9.mol
WNK463 Property
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO : ≥ 30 mg/mL (64.73 mM)
- pka
- 15.18±0.46(Predicted)
N-Bromosuccinimide Price
- Product number
- SML2809
- Product name
- WNK463
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $118
- Updated
- 2024/03/01
- Product number
- SML2809
- Product name
- WNK463
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $453
- Updated
- 2024/03/01
- Product number
- W499305
- Product name
- WNK463
- Packaging
- 5mg
- Price
- $360
- Updated
- 2021/12/16
- Product number
- 6099EG
- Product name
- N-Tert-butyl-3-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]pyridin-2-yl]piperidin-4-yl]imidazole-4-carboxamide
- Packaging
- 10mg
- Price
- $378
- Updated
- 2021/12/16
- Product number
- CS-5921
- Product name
- WNK463
- Purity
- 99.55%
- Packaging
- 25mg
- Price
- $480
- Updated
- 2021/12/16
WNK463 Chemical Properties,Usage,Production
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.).