WNK inhibitor 12

WNK inhibitor 12 Property

storage temp. 

Store at -20°C

form 

Solid

color 

Off-white to light yellow

Hazard and Precautionary Statements (GHS)

WNK inhibitor 12 Chemical Properties,Usage,Production

Uses

WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].

Biological Activity

WNK-IN-11 D3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11 D3 is effective at regulating cardiovascular homeostasis[1]. WNK-IN-11 D3 (1.5 mg/kg; p.o.) shows an improved rat PK profile, including lower clearance, improvement in absolute oral exposure, and a 2-fold improvement in oral bioavailability[1].WNK-IN-11 D3 (30 mg/kg; p.o.) shows significant reductions in systolic blood pressure (SBP) vs untreated mice[1].WNK-IN-11 D3 (0~100 mg/kg; p.o.) induces dose dependent diuresis, natriuresis, and kaliuresis, from 10 to 100 mg/kg[1].WNK-IN-11 D3 shows trends toward reduction of blood pressure, stroke volume, and total peripheral resistance, while increasing heart rate. WNK-IN-11 D3 shows efficacy in rodent models of hypertension and volume overload[1].

in vivo

References

[1]. Yamada K, Levell J, Yoon T, et al. Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models. J Med Chem. 2017;60(16):7099-7107.