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.
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- CAS No.: 851220-34-3
- Formule: C12H19NO3S2
- Masse moléculaire:289.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
Chemical Information
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CAS No. 851220-34-3
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Masse moléculaire 289.41
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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