WNK inhibitor 12
WNK inhibitor 12 Basic information
- Product Name:
- WNK inhibitor 12
- Synonyms:
-
- WNK inhibitor 12
- WNK 476
- WNK-476
- WNK IN 12
- WNKIN12
- WNK-IN-12
- WNK-IN-11-d3
- WNK IN 11 d3,WNK-IN-11-d-3,WNKIN11d3
- CAS:
- 2123483-49-6
- MF:
- C21H21Cl2N5OS
- MW:
- 462.39
- Mol File:
- 2123483-49-6.mol
WNK inhibitor 12 Chemical Properties
- storage temp.
- Store at -20°C
- form
- Solid
- color
- Off-white to light yellow
WNK inhibitor 12 Usage And Synthesis
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.