BAY 41-8543 是口服有效的，不依赖一氧化氮 (NO) 的可溶性鸟苷酸环化酶 (sGC) 的刺激物。BAY 41-8543 在大鼠的肺和全身血管床中具有血管舒张活性。BAY 41-8543 具有抗血小板作用，并有用于心血管疾病研究的潜力。
| 生物活性 | BAY 41-8543 is an orally active, nitric oxide (NO)-independent stimulator ofsoluble guanylyl cyclase (sGC). BAY 41-8543 has vasodilator activity in the pulmonary and systemic vascular beds in the rat. BAY 41-8543 has antiplatelet effects and has the potential for cardiovascular diseases research[1]. |
体内研究
(In Vivo) | BAY 41-8543 (10-100 μg/kg; IV) produces small decreases in pulmonary arterial pressure, larger dose-dependent decreases in systemic arterial pressure, and increases in cardiac output[1].
BAY 41-8543 (0.003, 0.01, 0.03, 0.1, and 0.3 mg/kg; iv) produces a dose-dependent and long-lasting decrease in blood pressure in anaesthetized rats. The blood pressure lowering effect of BAY 41-8543 lasts longer than the observation period of 30 min. BAY 41-8543 (0.1, 0.3 and 1.0 mg kg; oral) has maximal blood pressure lowering effects. The blood pressure lowering effects of the highest doses of BAY41-8543 lasts longer than the observation period of 120 min[2].
BAY 41-8543 (3 mg/kg; p.o.; twice daily; for 5 weeks) completely prevents the development of the increase in systolic blood pressure in 18-week-old renin transgenic rats (TGR(mRen2)27) on L-NAME treatment. BAY 41-8543 dramatically increases survival[2].
| Animal Model: | Adult male Sprague-Dawley rats weighing 325-450 g[1] | | Dosage: | 10, 30, and 100 μg/kg | | Administration: | IV | | Result: | Produced small decreases in pulmonary arterial pressure, larger dose-dependent decreases in systemic arterial pressure, and increases in cardiac output. |
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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: DMF : 16.67 mg/mL(39.65 mM;Need ultrasonic) Ethanol : 1 mg/mL(2.38 mM;ultrasonic and warming and heat to 70℃) DMSO :< 1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble or slightly soluble) 配制储备液 | 1 mM | 2.3785 mL | 11.8923 mL | 23.7846 mL | | 5 mM | 0.4757 mL | 2.3785 mL | 4.7569 mL | | 10 mM | 0.2378 mL | 1.1892 mL | 2.3785 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。 |
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