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WNK463

WNK463 Struktur
2012607-27-9
CAS-Nr.
2012607-27-9
Englisch Name:
WNK463
Synonyma:
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
Summenformel:
C21H24F3N7O2
Molgewicht:
463.46
MOL-Datei:
2012607-27-9.mol

WNK463 Eigenschaften

Dichte
1.43±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
L?slichkeit
DMSO : ≥ 30 mg/mL (64.73 mM)
pka
15.18±0.46(Predicted)
Aggregatzustand
Solid
Farbe
White to off-white

Sicherheit

WNK463 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

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.).

WNK463 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


WNK463 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 68)Lieferanten
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ATK CHEMICAL COMPANY LIMITED
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Wuhan Jingkang en Biomedical Technology Co., Ltd
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orders@jknbiochem.com China 5221 58
SHANGHAI KEAN TECHNOLOGY CO., LTD.
+8613817748580
cooperation@kean-chem.com China 40066 58

  • WNK463
  • WNK 463;WNK-463
  • CS-2515
  • 1H-Imidazole-5-carboxamide, N-(1,1-dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-
  • Ser/Thr Protease,WNK 463,inhibit,WNK463,Serine proteases,Inhibitor,Serine endopeptidases,Threonine proteases,WNK-463
  • 2012607-27-9
  • C21H24F3N7O2
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