CP 71362
CP 71362 is a renin inhibitor, a highly potent substrate-analog transition state mimic with antihypertensive properties. CP 71362 exhibits significant inhibitory activity against plasma renin from rats, dogs, and humans (IC50 values are 3 nM, 0.0033 nM, and 20 nM, respectively). CP 71362 reduces the mean arterial pressure of anesthetized and conscious sodium-depleted animals in a dose-dependent manner, and has pharmacokinetic characteristics of rapid elimination and short duration of action. CP 71362 can be used in research related to hypertension and congestive heart failure.
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- CAS No.: 112227-15-3
- 화학식: C51H76N8O9
- 분자량:945.20
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보관:
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
CP-71,362 exhibits high specificity for renin, with a potency 6 orders of magnitude lower against bovine spleen cathepsin D (IC50=1.3×10-6 M), and shows no inhibitory activity against rabbit lung ACE at concentrations up to 1×10-3 M[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CP 71362 (9.7-30 μg/kg/min; i.v.; continuous infusion) reduces mean arterial pressure in conscious, sodium-depleted Sprague-Dawley rats, with an ED50 infusion rate of 9.7 μg/kg/min and a 30-40 mmHg pressure decrease at 30 μg/kg/min[1].
CP 71362 (0.1-3 mg/kg; i.v. bolus) produces dose-dependent mean arterial pressure lowering in conscious, sodium-depleted Cavia porcellus, with the 1.0 and 3.0 mg/kg bolus doses maintaining significant effects for at least 2 hours[2].
CP 71362 (1.06-100 μg/kg/min; i.v. infusion; 10-30 minutes) produces dose-dependent, reversible mean arterial pressure lowering in anesthetized, sodium-depleted dogs, with an ED50 of 1.06 μg/kg/min, and completely suppresses plasma renin activity at the ED50 dose[2].
CP 71362 (4.3-43.3 μg/kg/min; i.v. infusion; 30 minutes) produces rapid, dose-dependent, fully reversible mean arterial pressure lowering in conscious, sodium-depleted SHR, with an ED50 of 5 μg/kg/min[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:(anesthetized, sodium-depleted)[1]
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Dosage:1.1 μg/kg/min (ED50 infusion rate); 3.7 ± 0.4 μg/kg/min; 4.5 ± 0.7 μg/kg/min
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Administration:i.v.; continuous infusion
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Result:Reduced mean arterial pressure by 35 mmHg (from 119 mmHg to 84 mmHg, n=5).
Achieved an ED50 infusion rate of 1.1 μg/kg/min for half-maximal decrease in renin-dependent blood pressure.
Produced near-maximal effects on mean arterial pressure at 4.5 ± 0.7 μg/kg/min (~4× the ED50 dose).
Returned mean arterial pressure to pre-infusion levels within 30-60 minutes after cessation of infusion.
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Animal Model:Sprague-Dawley (conscious, sodium-depleted)[1]
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Dosage:9.7 μg/kg/min (ED50 infusion rate); 30 μg/kg/min
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Administration:i.v.; continuous infusion
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Result:Reduced mean arterial pressure by 30-40 mmHg at 30 μg/kg/min.
Achieved an ED50 infusion rate of 9.7 μg/kg/min for half-maximal fall in renin-dependent blood pressure.
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Animal Model:Charles River (300-350g; sodium-depleted, renin-dependent hypertension model)[2]
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Dosage:0.1 mg/kg; 1.0 mg/kg; 3.0 mg/kg
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Administration:i.v. bolus
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Result:Caused a maximum mean arterial pressure decrease of 32 ± 5 mmHg, with significant lowering sustained for 60 minutes at 0.1 mg/kg.
Caused a maximum mean arterial pressure decrease of 36 ± 3 mmHg, with significant lowering sustained for at least 120 minutes at 1.0 mg/kg.
Caused a maximum mean arterial pressure decrease of 38 ± 1 mmHg, with significant lowering sustained for at least 120 minutes at 3.0 mg/kg.
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Animal Model:Mongrel (10-15 kg; sodium-depleted, renin-dependent hypertension model)[2]
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Dosage:1.06 µg/kg/min; 4.52 µg/kg/min; 5.0 µg/kg/min; 10.0 µg/kg/min; 20.0 µg/kg/min; 50.0 µg/kg/min; 100.0 µg/kg/min
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Administration:i.v. infusion; 30 minutes (most doses); 10 minutes (4.52 µg/kg/min)
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Result:Caused dose-dependent lowering of mean arterial pressure, with a maximum decrease of ~50 mmHg at 10.0 µg/kg/min.
Achieved an ED50 of 1.06 µg/kg/min for mean arterial pressure lowering.
Reduced mean arterial pressure from ~115 mmHg to 80 mmHg at 4.52 µg/kg/min, with pressure returning to pre-infusion levels approximately 1 hour after infusion termination.
Reduced plasma renin activity from 23.8 ± 2.5 to 0.04 ± 0.01 ng AngI/mL/hr (p < 0.01) at 1.11 µg/kg/min (ED50 dose).
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Animal Model:Spontaneously Hypertensive Rats (SHR) (Charles River, 275-300 g; sodium-depleted, renin-dependent hypertension model)[2]
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Dosage:4.3 µg/kg/min; 10.8 µg/kg/min; 43.3 µg/kg/min
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Administration:i.v. infusion; 30 minutes
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Result:Caused dose-dependent mean arterial pressure lowering, with a maximum decrease of 43 mmHg at 43.3 µg/kg/min.
Achieved an ED50 of 5 µg/kg/min for mean arterial pressure lowering.
Reached a stable nadir within 10-20 minutes of starting infusion, with pressure returning to baseline within 5 minutes of stopping infusion.
Chemical Information
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CAS No. 112227-15-3
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분자량 945.20
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화학식 C51H76N8O9
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SMILES
O=C([C@@H](NC(OC(C)(C)C)=O)CC1=CC=CC=C1)N[C@H](C(N[C@@]([H])(CC2CCCCC2)[C@@H](O)C[C@H](C(N[C@H](C(N[C@H](C(O)=O)CC3=CC=CC=C3)=O)CCCCN)=O)CC(C)C)=O)CC4=CNC=N4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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