NI929
NI929 is a blood-brain barrier-permeable recombinant mouse aminopeptidase A (APA) inhibitor with a Ki value of 30 nM. NI929 is applicable to research on hypertension and Alzheimer's disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 851220-34-3
- 分子式: C12H19NO3S2
- 分子量:289.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
NI929 potently inhibits the activity of recombinant mouse aminopeptidase A, with a Ki value of 30 nM[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar Kyoto (WKY) (10-week-old male; deoxycorticosterone acetate-salt induced hypertension)[1]
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Dosage:25 µg (intracerebroventricular)
0.3, 1, 2, 4, 15 mg/kg (intravenous)
4 mg/kg (oral) -
Administration:intracerebroventricular; single dose; intravenous; single dose; p.o.; single dose
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Result:Lowered MABP dose-dependently, intravenous ED50 = 0.53 mg/kg.
Oral 4 mg/kg normalized MABP to WKY baseline: -44 mmHg peak at 4 h, -21 mmHg at 10 h, full recovery at 24 h.
Suppressed brain APA activity via intracerebroventricular, intravenous and oral routes.
Oral 4 mg/kg lowered plasma AVP and raised diuresis and natriuresis within 5 h.
Kept plasma sodium and potassium stable at all time points.
Altered no APA, MABP, AVP, diuresis, natriuresis in normotensive WKY rats and exerted no heart rate effects in all rats.
化学情報
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CAS 番号 851220-34-3
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分子量 289.41
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分子式 C12H19NO3S2
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SMILES
O=S(CC[C@H](N)[C@@H](S)CCC1=CC=CC=C1)(O)=O
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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]. Keck M, et al. NI956/QGC006, a Potent Orally Active, Brain-Penetrating Aminopeptidase A Inhibitor for Treating Hypertension. Hypertension (Dallas, Tex. : 1979). 2019 Jun;73(6):1300-1307. [Content Brief]
[2]. Loera-Valencia R, et al. Brain Renin-Angiotensin System as Novel and Potential Therapeutic Target for Alzheimer's Disease. International journal of molecular sciences. 2021 Sep 20;22(18):10139. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)