KRI-1177
KRI-1177 is a competitive, dipeptide human renin inhibitor with a Ki of 0.7 μM and an IC50 of 90 nM. The IC50 of KRI-1177 targeting cynomolgus monkey renin is 680 nM. KRI-1177 acts as an antihypertensive agent, angiotensin inhibitor and plasma renin activity inhibitor, which reduces systemic blood pressure and plasma angiotensin concentration. KRI-1177 exhibits a relatively long-lasting antihypertensive effect in cynomolgus monkeys and can be used for hypertension research.
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- CAS No.: 105186-68-3
- Formule: C37H45N5O6
- Masse moléculaire:655.80
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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
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Activité biologique
Description
In Vitro
KRI-1177 (0.5 μM; 30 min) potently and selectively inhibits primate (human, Japanese monkey) plasma renin activity in vitro, with competitive inhibition of purified human renin (Ki = 0.7 μM), and far weaker inhibition of non-primate plasma renin and other proteolytic enzymes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KRI-1177 (0.1-5 mg/kg; i.v.; single bolus injection) produces only a slight, transient hypotensive effect (~12 mmHg fall in mean blood pressure at 5 mg/kg i.v.) in anesthetized Japanese monkeys on a normal diet[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Japanese monkey (Macaca fuscata) (both sexes, 6-9 kg, hypertension model via low sodium diet for 1 week, furosemide pretreatment, anesthetized with pentobarbital sodium)[1]
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Dosage:0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 2.5 mg/kg; 5 mg/kg
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Administration:i.v.; single bolus injection
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Result:Produced a dose-dependent fall in systemic blood pressure.
Attained maximal hypotensive response of ~25 mmHg fall in mean blood pressure 5 minutes after 5 mg/kg i.v. injection, with half-maximal response restoration time of approximately 15 minutes.
Reduced plasma renin activity from pre-treatment mean of ~28 ng ANG I/mL per h to ~10 ng ANG I/mL per h after 1 mg/kg i.v. injection.
Reduced plasma renin activity from pre-treatment mean of ~50 ng ANG I/mL per h to ~5 ng ANG I/mL per h after 5 mg/kg i.v. injection.
Decreased plasma ANG I concentrations by 51.4% (from 1.62 ng/mL to 0.72 ng/mL) after 5 mg/kg i.v. injection.
Decreased plasma ANG II + III concentrations by 49.6% (from 149 pg/mL to 72 pg/mL) after 5 mg/kg i.v. injection.
Did not significantly alter heart rate at 5 mg/kg i.v.
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Animal Model:Japanese monkey (Macaca fuscata) (both sexes, 6-9 kg, normotensive, fed normal diet, anesthetized with pentobarbital sodium)[1]
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Dosage:0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 2.5 mg/kg; 5 mg/kg
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Administration:i.v.; single bolus injection
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Result:Induced a slight and transient fall in systemic blood pressure.
Attained maximal hypotensive response of ~12 mmHg fall in mean blood pressure 2 minutes after 5 mg/kg i.v. injection.
Chemical Information
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CAS No. 105186-68-3
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Masse moléculaire 655.80
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Formule C37H45N5O6
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SMILES
O=C(OC)C(O)C(NC(=O)C(NC(=O)C(CC(=O)NCCC=1C=CC=CC1)CC2=CC=CC=3C=CC=CC32)CC4=CN=CN4)CC(C)C
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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)
KRI-1177 Related Classifications
HY-119036 Related Classifications
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