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Lisinopril dihydrate RAAS inhibitor

Cat.No.S2076

Lisinopril dihydrate(MK-521 dihydrate) is an angiotensin-converting enzyme (ACE) inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications of diabetes.
Lisinopril dihydrate RAAS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 441.52

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Chemical Information, Storage & Stability

Molecular Weight 441.52 Formula

C21H35N3O7

 Storage (From the date of receipt)
CAS No. 83915-83-7 Download SDF Storage of Stock Solutions

Synonyms MK-521 dihydrate Smiles C1CC(N(C1)C(=O)C(CCCCN)NC(CCC2=CC=CC=C2)C(=O)O)C(=O)O.O.O

Solubility

In vitro
Batch:

Water : 88 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight

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

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Mechanism of Action

Targets/IC50/Ki
ACE [1]
In vitro

Lisinopril significantly reduces left ventricular (LV) end-diastolic pressure (EDP), pulmonary capillary wedge pressure (PCWP) and end-diastolic stress, addition of atenolol to Lisinopril further reduces EDP and PCWP. [1] Lisinopril is a structural homologue of enalaprilat, differing only in the second amino acid side chain. Lisinopril inhibits Angiotensin-converting enzyme (ACE) in vitro, as well as after parenteral and oral administration to humans; its oral bioavailability is only 25-29%, but it has a longer duration of action than enalapril. [2]
In vivo

Lisinopril treated SHR rats has significantly raised total cholesterol levels compared to untreated spontaneously hypertensive rats (SHR) rats (+27%), but not compared to lisinopril treated Wistar Kyoto rats (WKY) rats. [3] Lisinopril is a long-acting angiotensin-converting enzyme inhibitor which blocks the renin-angiotensin system (RAS) and reduces systemic blood pressure in rats. Lisinopril reduces the hydroxyproline level and inhibits accumulation of collagens in the pulmonary tissue of the treatment group (paraquat + lisinopril) and per-treatment group (lisinopril + paraquat) in rats. [4] Lisinopril results in preserved ultrafiltration volume (UF), glucose reabsorption (D 1 /D 0 glucose) and peritoneal thickness in rats. [5] Lisinopril (0.2 mg/kg twice a day for 10 days) protects the cell membrane integrity and lessens free radical-induced oxidant stress in guinea pig hearts. [6]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16458281/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15770604/
  • [6] https://pubmed.ncbi.nlm.nih.gov/10814965/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05061901 Completed
Bioequivalence
Pharmtechnology LLC|ClinPharmInvest LLC
 October 6 2021 Phase 1
NCT03599466 Unknown status
Healthy
Bright Future Pharmaceuticals Factory O/B Bright Future Pharmaceutical Laboratories Limited|Chinese University of Hong Kong
 October 2019 Phase 1

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