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.

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].

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].

[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.

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