SPH3127 (DRI 18) 是一种新型的、高度有效的、且具有口服活性的direct renin抑制剂 (recombinant human-reninIC50=0.4 nM，human plasma renin activityIC50=0.45 nM)。SPH3127 具有抗高血压作用，可用于高血压的研究。
| 生物活性 | SPH3127 (DRI 18) is a novel, highly potent, and orally activedirectrenininhibitor (recombinant human-reninIC50=0.4 nM, human plasmareninactivityIC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research[1]. |
体内研究
(In Vivo) | SPH3127 (oral administration; 0-10 mg/kg; once) shows favorable bioavailability in cynomolgus monkeys[1].
SPH3127 (oral administration; 0-3 mg/kg; once) shows a hypotensive effect on tsukuba hypertensive mice[1].
| Animal Model: | Cynomolgus monkeys pretreated with a low-sodium diet and furosemide[1] | | 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 IC50value of 0.46 nM, and showed hypotensive effect. |
| Animal Model: | Tsukuba hypertensive mice (THM)[1] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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