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Technical Data
| Formula | C44H44CaN2O8S4 |
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| Molecular Weight | 897.17 | CAS No. | 81938-43-4 | |
| Solubility (25°C)* | In vitro | DMSO | 5.33 mg/mL (5.94 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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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. | |
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| 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)
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.