Zofenopril calcium

Catalog No.S5712 Synonyms: SQ-26991

For research use only.

Zofenopril calcium (SQ-26991) is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure.

Zofenopril calcium Chemical Structure

CAS No. 81938-43-4

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Biological Activity

Description Zofenopril calcium (SQ-26991) is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure.
Targets
ACE [1]
()
In vitro

In guinea pig ileum zofenopril inhibited the contractile response to angiotensin I and augmented the contractile response to bradykinin. The EC50 of zofenoprilat was in the nanomolar range (1-8 nM). In homogenates of aorta, brain, heart, lung, kidney, and serum of spontaneously hypertensive rats (SHRs), zofenoprilat inhibited ACE with a very similar potency (IC50: 0.8-2.8 nM). Zofenoprilat (0.01-1 mM) was shown to protect endothelial function. It abolished the proapoptotic effects of doxorubicin, promoted mitosis of bovine coronary venular endothelial cells (CVEC), enhanced concentration-dependently cell survival, and improved VEGF-induced proliferation of CVECs (kept 5 days in 0.1% serum to mimic a stress condition). Zofenoprilat (1-100 μM) also promoted angiogenesis in porcine coronary arteries. Zofenoprilat appears to favor proliferation of coronary endothelial cells, leading to angiogenesis by reversing apoptosis[1].

In vivo In conscious rats, dogs, and monkeys, oral administration of zofenopril (0.03-0.6 mg/kg) induces a dose-dependent inhibition of the pressor response to angiotensin I. It does not antagonize the effects of angiotensin II or other spasmogens. In 2K-1C rats, zofenopril produces a dose-dependent antihypertensive effect of long duration (>17 h). At 6.6 mg/kg, zofenopril lowered blood pressure by as much as 70 mmHg (220 to 150 mmHg). In SHRs, zofenopril has dose-dependent effects, lowering of blood pressure by 21-33 mmHg. At the highest dose used, zofenopril lowers blood pressure for at least 17 h. The effects of repeated administration of 22 mg/kg zofenopril b.i.d. were evaluated in SHRs. Systolic blood pressure (SBP) fell by 47 mmHg (188 to 141 mmHg) by day 14 of the study. The duration of the effect was longer than 12 h as identical SBP values were recorded at either 1 or 12 h after drug administration. Based on urinary excretion after oral and i.v. administration, the oral absorption of zofenopril was estimated to exceed 80% in rats and dogs and 70% in monkeys. The bioavailability of zofenoprilat after an oral dose of zofenopril was 100% in rats, >70% in dogs, and 50% in monkeys. Based on a comparison of AUC values after oral and i.v. administration, the oral absorption of [14C]zofenopril in dogs was 100% and the bioavailability of zofenoprilat was 93%. Following an oral administration of zofenopril, Tmax values for zofenoprilat were between 0.3-0.9 h and T1/2 values between 5–7 h for either of the three animal species. In dogs receiving zofenopril by intraarterial, intravenous, intraportal, or oral routes, 95% of the orally administered dose of zofenopril was hydrolyzed during the first pass[1].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 5.33 mg/mL warmed
(5.94 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 897.17
Formula

C44H44CaN2O8S4

CAS No. 81938-43-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(CSC(=O)C1=CC=CC=C1)C(=O)N2CC(CC2C(=O)[O-])SC3=CC=CC=C3.CC(CSC(=O)C1=CC=CC=C1)C(=O)N2CC(CC2C(=O)[O-])SC3=CC=CC=C3.[Ca+2]

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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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