Indolapril
Indolapril (CI-907) is an orally active angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 80 nM. Indolapril exerts a highly specific functional inhibitory effect on Ang I-mediated pressor/contractile responses, and its antihypertensive effect correlates with ACE inhibition in vascular tissues. Indolapril reduces blood pressure in multiple rodent and canine models of hypertension. Indolapril exists as a monoester prodrug and an active diacid form, and no side effects are observed in tested conscious animals. Indolapril is applicable to hypertension-related research.
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- CAS No.: 80876-01-3
- Formule: C24H34N2O5
- Masse moléculaire:430.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
In Vitro
Indolapril (compound 11a) has an IC50 of 80 nM in the in vitro angiotensin-converting enzyme (ACE) inhibition assay[1].
Indolapril potently inhibits angiotensin-converting enzyme (ACE) in guinea pig serum, and its diacid form exhibits higher potency (IC50 = 2.6 nM) than its monoester prodrug form (IC50 = 170 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Indolapril (0.03-30 mg/kg; p.o.; once daily) exerts a dose-dependent antihypertensive effect in two-kidney, one-clip Goldblatt hypertensive rats[2].
Indolapril (30 mg/kg; p.o.; once daily; for 5 consecutive days) reduces blood pressure in spontaneously hypertensive rats, and the magnitude of its hypotensive effect is comparable to its effect in renal hypertensive rats[2].
Indolapril (10 mg/kg; p.o.; single administration) normalizes blood pressure in diuretic-pretreated dogs with renal hypertension[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:conscious two-kidney one-clip Goldblatt renal hypertensive rats were measured for blood pressure in the unanesthetized state[1]
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Dosage:0.1, 0.3, 1.0, 10.0 and 30.0 mg/kg
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Administration:p.o.; single dose
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Result:Decreased mean aortic blood pressure in a dose-dependent manner from baseline values of 185-197 mmHg by 52, 73, 72, 86 and 102 mmHg at 0.1, 0.3, 1.0, 10.0 and 30.0 mg/kg, respectively.
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Animal Model:spontaneously hypertensive rats[2]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 5 days
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Result:Produced a decrease in blood pressure equivalent to that seen in renal hypertensive rats treated with indolapril.
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Animal Model:diuretic-pretreated renal hypertensive dogs[2]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Normalized blood pressure.
Showed lower heart rate increases compared to Enalapril (HY-B0331) -treated dogs for equivalent blood pressure reductions.
Chemical Information
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CAS No. 80876-01-3
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Masse moléculaire 430.54
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Formule C24H34N2O5
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SMILES
CCOC([C@H](CCC1=CC=CC=C1)N[C@@H](C)C(N2[C@]3([H])[C@](CCCC3)([H])C[C@H]2C(O)=O)=O)=O
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Synonyms
CI-907
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Indolapril Related Classifications
HY-187710 Related Classifications
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