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| | 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 | | EINECS: | | | Product Categories: | | | 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 |
| 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 | 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: | SpragueDawley rats[1] | | Dosage: | 1.5 mg/kg | | Administration: | P.o. | | Result: | Showed an improved rat PK profile, including lower clearance, improvement in absolute oral exposure, and a 2-fold improvement in oral bioavailability.
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| Animal Model: | FVB mice[1] | | Dosage: | 30 mg/kg | | Administration: | P.o. | | Result: | Showed significant reductions in systolic blood pressure (SBP) vs untreated mice.
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| Animal Model: | FVB mice[1] | | Dosage: | 0~100 mg/kg | | Administration: | P.o. | | Result: | Induced dose dependent diuresis, natriuresis, and kaliuresis, from 10 to 100 mg/kg.
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| | 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. |
| | WNK inhibitor 12 Preparation Products And Raw materials |
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