Bioactivity | 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]. | ||||||||||||
Target | WNK | ||||||||||||
In Vivo | 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]. Animal Model: | ||||||||||||
Name | WNK-IN-11-d3 | ||||||||||||
CAS | 2123483-49-6 | ||||||||||||
Formula | C21H18D3Cl2N5OS | ||||||||||||
Molar Mass | 465.41 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |