Prorenone
Prorenone (SC 23133) is a spironolactone-type steroidal mineralocorticoid receptor (MR) antagonist that can cross the blood-brain barrier, with low affinity for glucocorticoid receptors and rat prostate androgen receptors. Prorenone inhibits the binding and action of Aldosterone (HY-113313), blocks its induced nuclear receptor activity and stimulated sodium transport, antagonizes aldosterone-induced urinary potassium excretion, and prevents aldosterone-induced elevation of blood pressure. Prorenone can be used in research related to hypertension.
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- CAS 番号: 40574-52-5
- 分子式: C23H30O3
- 分子量:354.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
Prorenone exhibits slightly higher binding affinity for renal mineralocorticoid receptors than aldosterone in vitro, and shows higher specificity for mineralocorticoid receptors over glucocorticoid receptors and androgen receptors compared with Spironolactone (HY-B0561)[1].
Prorenone binds to a single class of specific sites with high affinity and low capacity in soluble renal proteins from the kidneys of adrenalectomized male Wistar rats, with a mean dissociation constant (Kd) of 1.54 nM[2].
Prorenone (1-10 nM; 20-60 min) forms cytosolic complexes with renal receptors in kidney homogenates from adrenalectomized male Wistar rats, but these complexes do not translocate to the nucleus, and exert an equivalent inhibitory effect on both cytosolic and nuclear binding of aldosterone[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Prorenone (1.5 mg; i.p.; single dose) significantly antagonizes aldosterone-induced kaliuresis in adrenalectomized rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, initial weight ~300 g, unilaterally nephrectomized, intracerebroventricular aldosterone infusion-induced hypertension)[1]
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Dosage:0.005 μg/h; 0.02 μg/h
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Administration:intracerebroventricularly; continuous infusion; 30 days
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Result:Blocked aldosterone-induced systolic blood pressure elevation, with final systolic blood pressure of 133 mmHg (0.005 μg/h coadministered with aldosterone) and 139 mmHg (0.02 μg/h coadministered with aldosterone), both not significantly different from control (132 mmHg), compared to aldosterone-only group's 149 mmHg.
Resulted in final systolic blood pressure of 136 mmHg when administered alone at 0.02 μg/h, not significantly different from controls.
Showed no significant differences in urine volume, body weight, or heart, kidney, or adrenal gland weight-to-body weight ratios between prorenone-treated groups and controls.
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Animal Model:Wistar rats (male, 180-200 g, adrenalectomized 2-5 days prior)[2]
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Dosage:1.5 mg
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Administration:i.p.; single dose
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Result:Reversed aldosterone-induced kaliuresis, resulting in a mean urinary K+ excretion of 0.45 meq over 5 hours.
Increased mean log Na+:K+ ratio to 0.46.
化学情報
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CAS 番号 40574-52-5
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分子量 354.49
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分子式 C23H30O3
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SMILES
C[C@@]12[C@]3(CC[C@]1([C@]4([C@](CC2)([C@]5(C)C([C@]6([C@@]4(C6)[H])[H])=CC(=O)CC5)[H])[H])[H])OC(=O)CC3
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別名
SC 23133
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Gomez-Sanchez EP, et al. Intracerebroventricular infusion of aldosterone induces hypertension in rats. Endocrinology. 1986 Feb;118(2):819-23. [Content Brief]
[2]. Claire M, et al. Mechanism of action of a new antialdosterone compound, prorenone. Endocrinology. 1979 Apr;104(4):1194-200. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Prorenone 関連分類
HY-106593 関連分類
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- Prorenone
- 40574-52-5
- SC 23133
- SC23133
- SC-23133
- Mineralocorticoid Receptor
- toad bladder preparations
- ventral prostate proteins
- renal proteins
- mineralocorticoid receptor
- orchidectomized male Wistar rats
- androgen receptor
- hypertension
- adrenalectomized male Wistar rat kidneys
- aldosterone
- glucocorticoid receptor
- Inhibitor
- inhibitor
- inhibit