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Imidaprilate

Names

[ CAS No. ]:
89371-44-8

[ Name ]:
Imidaprilate

[Synonym ]:
(4S)-3-<(2S)-2-<N-((1S)-1-carboxy-3-phenylpropyl)amino>propionyl>-1-methyl-2-oxoimidazolidine-4-carboxylic acid
(4S)-1-methyl-3-{(2S)-2-[N-((1S)-1-carboxy-3-phenylpropyl)amino]propionyl}-2-oxo-imidazolidine-4-carboxylic acid
UNII-WUU07Y30IA
Imidapril Diacid
Imidaprilat
(4S)-3-[(2S)-N-[(1S)-1-carboxy-3-phenylpropyl]alanyl]-1-methyl-2-oxoimidazolidine-4-carboxylic acid

Biological Activity

[Description]:

Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Angiotensin-converting Enzyme (ACE)
Research Areas >> Cardiovascular Disease

[Target]

IC50: 2.6 nM (ACE)[1]


[In Vitro]

Imidaprilate (6366A) is an active metabolite of 6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM. Imidaprilate augments the bradykinin-induced contraction of guinea pig ileum, with AC50 of 1.7 nM[1].

[In Vivo]

Imidaprilate (≥0.2 mg/kg) inhibits angiotensin I (AT-I)-induced pressor response. TA-6366 lowers the blood pressure in two-kidney one-clip renal hypertensive rats at 0.5-2 mg/kg via oral administration, and in spontaneously hypertensive rats (SHRs) at 2 to 10 mg/kg[1].

[References]

[1]. Kubo M, et al. Pharmacological studies on (4S)-1-methyl-3-[(2S)-2-[N-((1S)-1-ethoxycarbonyl-3-phenylpropyl)amino] propionyl]-2-oxo-imidazolidine-4-carboxylic acid hydrochloride (TA-6366), a new ACE inhibitor: I. ACE inhibitory and anti-hypertensive activities. Jpn J Pharmacol. 1990 Jun;53(2):201-10.


[Related Small Molecules]

Angiotensin I/II (1-7) trifluoroacetate salt | Captopril | Enalapril maleate | Perindopril erbumine | Lisinopril diydrate | Phosphoramidon disodium salt | Trandolapril | Fosinopril sodium | Quinapril hydrochloride | Ramipril | Cilazapril Monohydrate | Enalaprilat Dihydrate | omapatrilat | Temocapril (hydrochloride) | Hemorphin-7

Chemical & Physical Properties

[ Melting Point ]:
180-182ºC

[ Molecular Formula ]:
C18H23N3O6

[ Molecular Weight ]:
377.39200

[ Exact Mass ]:
377.15900

[ PSA ]:
127.25000

[ LogP ]:
0.66440

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream