WNK-IN-11 D3 是一种具有口服活性、选择性和强效的 With-No-Lysine (WNK) 激酶抑制剂。WNK-IN-11 D3 有效调节心血管稳态。
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]. |
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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].
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. |
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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 |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(214.86 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.1486 mL | 10.7432 mL | 21.4864 mL | 5 mM | 0.4297 mL | 2.1486 mL | 4.2973 mL | 10 mM | 0.2149 mL | 1.0743 mL | 2.1486 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |