产品
编 号：F744759
分子式：C22H32N6O4
分子量：444.53
分子式：C22H32N6O4
分子量：444.53
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
询价
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10mg
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结构图
CAS No: 1399849-02-5
产品详情
生物活性：
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research.
体内研究：
SPH3127 (oral administration; 0-10 mg/kg; once) shows favorable bioavailability in cynomolgus monkeys.SPH3127 (oral administration; 0-3 mg/kg; once) shows a hypotensive effect on tsukuba hypertensive mice.Animal Model:Cynomolgus monkeys pretreated with a low-sodium diet and furosemide
Dosage:0, 1, 3, and 10 mg/kg
Administration:Oral administration; 1, 3, and 10 mg/kg; once
Result:Inhibited plasma renin activity with the IC50 value of 0.46 nM, and showed hypotensive effect.
Animal Model:Tsukuba hypertensive mice (THM)
Dosage:0, 0.3, 1, or 3 mg/kg
Administration:Oral administration; 0, 0.3, 1, or 3 mg/kg; once
Result:Exhibited a hypotensive effect on tsukuba hypertensive mice in a dose-dependent manner from 0.3 to 3 mg/kg, and showed a maximum hypotensive effect of approximately 30 mmHg at 2-3 h after administration at any dose.
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research.
体内研究：
SPH3127 (oral administration; 0-10 mg/kg; once) shows favorable bioavailability in cynomolgus monkeys.SPH3127 (oral administration; 0-3 mg/kg; once) shows a hypotensive effect on tsukuba hypertensive mice.Animal Model:Cynomolgus monkeys pretreated with a low-sodium diet and furosemide
Dosage:0, 1, 3, and 10 mg/kg
Administration:Oral administration; 1, 3, and 10 mg/kg; once
Result:Inhibited plasma renin activity with the IC50 value of 0.46 nM, and showed hypotensive effect.
Animal Model:Tsukuba hypertensive mice (THM)
Dosage:0, 0.3, 1, or 3 mg/kg
Administration:Oral administration; 0, 0.3, 1, or 3 mg/kg; once
Result:Exhibited a hypotensive effect on tsukuba hypertensive mice in a dose-dependent manner from 0.3 to 3 mg/kg, and showed a maximum hypotensive effect of approximately 30 mmHg at 2-3 h after administration at any dose.
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