product name Cilazapril Monohydrate
Description: Cilazapril Monohydrate is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure. Cilazapril is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat. It is known that the diacid form of Cilazapril is more potent that enalapril at inhibiting ACE.
References: J Pharmacol Sci. 2004 Jan;94(1):67-72; Life Sci. 1999;64(3):PL27-39.
435.51
Formula
C22H31N3O5.H2O
CAS No.
92077-78-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 87 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 87 mg/mL (199.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Kinase Assay: Cell Assay: |
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| In Vivo | Cilazapril (1 mg/kg, daily) tends to decrease and the higher dose (10 mg/kg, daily) significantly decreases systolic blood pressure (SBP) in subtotal nephrectomized rats. Cilazapril attenuates the further development of protein uria in a dose-dependent manner in subtotal nephrectomized rats. Cilazapril attenuates the increase in plasma fibrinogen concentration and serum albumin concentration in a dose-dependent manner. Cilazapril reduces serum MCP-1 concentration in the nephrectomized rats. Cilazapril decreases hepatic fibrinogen synthesis through the alleviation of the local inflammatory process and the improvement of hypoalbuminemia. Cilazapril normalizes systolic arterial pressure to 121 mm Hg (SD) in the treated SHR-SP rats. Cilazapril decreases systolic arterial pressure to a nearly normal level and prevents hypertensive retinal vascular changes, probably by improving endothelial function. Cilazapril results in a marked decrease in the Kd of the renal arginine vasopressin (AVP) receptor and an increase in the plasma AVP level in the spontaneously hypertensive rat. Cilazapril exerts a rapid, complete, and persistent antihypertensive effect in the spontaneously hypertensive rats (SHR) in vivo but has no effect on SAP in the normotensive Sprague-Dawley rat. Cilazapril treatment depresses heart performance (28-35%) in SHR but has no effect in the Sprague-Dawley rats. Cilazapril decreases blood pressure to control values and reduces HW:BW in hyperthyroid rats. |
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| Formulation & Dosage | |
| References | J Pharmacol Sci. 2004 Jan;94(1):67-72; Life Sci. 1999;64(3):PL27-39. |
