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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 112227-15-3
- Formule: C51H76N8O9
- Masse moléculaire:945.20
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
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.
-
Animal Model:(anesthetized, sodium-depleted)[1]
-
Dosage:1.1 μg/kg/min (ED50 infusion rate); 3.7 ± 0.4 μg/kg/min; 4.5 ± 0.7 μg/kg/min
-
Administration:i.v.; continuous infusion
-
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.
-
Animal Model:Sprague-Dawley (conscious, sodium-depleted)[1]
-
Dosage:9.7 μg/kg/min (ED50 infusion rate); 30 μg/kg/min
-
Administration:i.v.; continuous infusion
-
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.
-
Animal Model:Charles River (300-350g; sodium-depleted, renin-dependent hypertension model)[2]
-
Dosage:0.1 mg/kg; 1.0 mg/kg; 3.0 mg/kg
-
Administration:i.v. bolus
-
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.
-
Animal Model:Mongrel (10-15 kg; sodium-depleted, renin-dependent hypertension model)[2]
-
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
-
Administration:i.v. infusion; 30 minutes (most doses); 10 minutes (4.52 µg/kg/min)
-
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).
-
Animal Model:Spontaneously Hypertensive Rats (SHR) (Charles River, 275-300 g; sodium-depleted, renin-dependent hypertension model)[2]
-
Dosage:4.3 µg/kg/min; 10.8 µg/kg/min; 43.3 µg/kg/min
-
Administration:i.v. infusion; 30 minutes
-
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
-
CAS No. 112227-15-3
-
Masse moléculaire 945.20
-
Formule C51H76N8O9
-
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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
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)
CP 71362 Related Classifications
HY-182301 Related Classifications
Powered by Bioz