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Moexipril hydrochloride

CAS: 82586-52-5 F: C27H35ClN2O7 W: 535.03

Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes eff
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Bioactivity Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril hydrochloride exhibits antihypertensive and neuroprotective effects[1]-[4].
Target IC50: 2.1 nM (purified ACE from rabbit lung), 1.75 nM (ACE in rat plasma)
Invitro Moexipril hydrochloride is devoid of anti-inflammatory properties and has no effect on platelet function[2].Moexipril hydrochloride hydrolyzes to Moexiprilat, and Moexiprilat inhibits ACE in guinea pig serum as well as on purified ACE from rabbit lung with IC50s of 2.6 and 4.9 nM, respectively[2].Moexipril hydrochloride (0.01 nM-0.1 mM) exhibits high potency against both plasma ACE and purified ACE from rabbit lung, with IC50s of 2.7 mM and 0.165 mM, respectively[3].Moexipril hydrochloride (0-100 μM, 24 h) significantly reduced the percentage of damaged neurons in a dose-dependent manner[4]. Moexipril hydrochloride (0-100 μM, 24 h) significantly attenuates Fe2+/3+-induced neurotoxicity[4].Moexipril hydrochloride dose not cause significant changes in the percentage of apoptotic neurons[4].
In Vivo Moexipril hydrochloride can not cross the blood-brain barrier[1].Moexipril hydrochloride (3 mg/kg, 30 mg/kg and 10 mg/kg, respectively; p.o.; once daily; 5 days) exhibits the a dose-dependent and antihypertensive effects in renal hypertensive rats, spontaneously hypertensive rats and perinephritic hypertensive dogs, respectively[3].Moexipril hydrochloride (0.3 mg/kg, i.p.) significantly reduces the infarct area on the mouse brain surface in NMRI mice[4].Moexipril hydrochloride (0.1 mg/kg, i.p.) significantly attenuates the cortical infarct volume in Long-Evans rats[4]. Animal Model:
Name Moexipril hydrochloride
CAS 82586-52-5
Formula C27H35ClN2O7
Molar Mass 535.03
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reference [1]. Chrysant, S.G. and G.S. Chrysant, Pharmacological and clinical profile of moexipril: a concise review. J Clin Pharmacol, 2004. 44(8): p. 827-36. [2]. Friehe H, et al. Pharmacological and toxicological studies of the new angiotensin converting enzyme inhibitor moexipril hydrochloride. Arzneimittelforschung. 1997 Feb. 47(2):132-44. [3]. Edling, O., et al., Moexipril, a new angiotensin-converting enzyme (ACE) inhibitor: pharmacological characterization and comparison with enalapril. J Pharmacol Exp Ther, 1995. 275(2): p. 854-63. [4]. Ravati A, et al. Enalapril and moexipril protect from free radical-induced neuronal damage in vitro and reduce ischemic brain injury in mice and rats. Eur J Pharmacol. 1999 May 28;373(1):21-33.