生物活性：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].
IC50 & Target：WNK[1]
体内研究(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].
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Sprague−Dawley 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.
Animal Model:
FVB mice[1]
Dosage:
30 mg/kg
Administration:
P.o.
Result:
Showed significant reductions in systolic blood pressure (SBP) vs untreated mice.
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.
分子量：465.41
Formula：C21H18D3Cl2N5OS
CAS 号：2123483-49-6
非标记 CAS：2123489-30-3
性状：固体
颜色：Off-white to light yellow
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Powder：-20°C：3 years，4°C：2 years
In solvent：-80°C：6 months，-20°C：1 month