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Cilazaprilat

Cilazaprilat structure

Cilazaprilat 

structure
  • CAS No:

    90139-06-3

  • Formula:

    C20H27N3O5

  • Chemical Name:

    Cilazaprilat

  • Synonyms:

    6H-Pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid,9-[[(1S)-1-carboxy-3-phenylpropyl]amino]octahydro-10-oxo-,(1S,9S)-;6H-Pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid,9-[(1-carboxy-3-phenylpropyl)amino]octahydro-10-oxo-,[1S-[1α,9α(R*)]]-;(1S,9S)-9-[[(1S)-1-Carboxy-3-phenylpropyl]amino]octahydro-10-oxo-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid;Ro 31-3113;Cilazaprilat

Description

White to Off-White Solid


Cilazaprilat is a non-proteinogenic alpha-amino acid.|Cilazaprilat is the active metabolite of cilazapril, a pyridazine angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, cilazapril is rapidly metabolized in the liver to cilazaprilat; cilazaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II, resulting in vasodilation. Cilazaprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.

Cilazaprilat Basic Attributes

389.452

389.45

WBL76FH528

DTXSID00238043

C75927

Characteristics

110

1.38370

White to off-white solid

1.34g/cm3

242 °C

618.9ºC at 760mmHg

328.1ºC

1.624

-20ºC Freezer

Drug Information

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|A class of drugs whose main indications are the treatment of hypertension and heart failure. They exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility. (See all compounds classified as Angiotensin-Converting Enzyme Inhibitors.)

cilazaprilat

Cilazaprilat Use and Manufacturing

The active metabolite of Cilazapril. An ACE inhibitor. Antihypertensive

Computed Properties

Molecular Weight:389.4
XLogP3:-2.4
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:7
Exact Mass:389.19507097
Monoisotopic Mass:389.19507097
Topological Polar Surface Area:110
Heavy Atom Count:28
Complexity:578
Defined Atom Stereocenter Count:3
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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