| Identification | Back Directory | [Name]
WNK inhibitor 12 | [CAS]
2123483-49-6 | [Synonyms]
WNK 476
WNK-476
WNKIN12
WNK-IN-12
WNK IN 12
WNK-IN-11-d3
WNK inhibitor 12 | [Molecular Formula]
C21H21Cl2N5OS | [MDL Number]
MFCD34567188 | [MOL File]
2123483-49-6.mol | [Molecular Weight]
462.39 |
| Hazard Information | Back Directory | [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]. | [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. |
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