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Delapril Hydrochloride RAAS inhibitor

Cat.No.S5728

Delapril Hydrochloride (Alindapril) is the hydrochloride salt form of delapril, which is a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.
Delapril Hydrochloride RAAS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 489

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S572801 DMSO]98 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 98.61%
98.61

Chemical Information, Storage & Stability

Molecular Weight 489 Formula

C26H33ClN2O5

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 83435-67-0 -- Storage of Stock Solutions

Synonyms Alindapril Hydrochloride Smiles CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N(CC(=O)O)C2CC3=CC=CC=C3C2.Cl

Solubility

In vitro
Batch:

DMSO : 98 mg/mL ( (200.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
ACE [1]
In vitro
The poteny of delapril is about 15 times greater than captopril and almost equal to enalaprilat in inhibiting rabbit lung ACE activity in vitro and about 10 times greater than captopril in inhibiting angiotensin I-induced contraction in isolated tissue preparations, such as rat aortic rings and rat kidney[2].
In vivo
After oral administration of [14C]delapril 10 mg/kg to rats, 57% of the dose is absorbed mainly in the small intestine via the portal route and extensively metabolized by esterases to the diacid derivative M-I. Plasma levels of M-I peak within 0.4 hour of administration (maximum concentration [Cmax] 1.23 μg/mL), then decline biphasically with half-lives of 0.6 and 9.1 hours. In dogs given 10 mg/kg of [14C]delapril, 72% of the dose is absorbed. Plasma levels of M-I peak within 0.4 hour of administration (Cmax, 0.9 μg/ mL), then decline biphasically with half-lives of 0.3 and 2.8 hours. Delapril is able to inhibit plasma and tissue ACE at doses 5-10 times lower than captopril and this has also been found in in vivo experiments. Delapril has been shown to decrease heart weight, left ventricular weight, the wall to lumen ratio of small coronary arterioles, and thickness of the left ventricular wall in stroke-prone SHR, to reduce cardiac renin gene expression in SHR, and to protect perfused rat hearts against ischemia-reperfusion injury[2].
References

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