Zofenopril calcium

製品コードS5712 バッチS571201

印刷

化学情報

Chemical Structure Synonyms SQ-26991 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C44H44CaN2O8S4
分子量 897.17 CAS No. 81938-43-4
Solubility (25°C)* 体外 DMSO 5.33 mg/mL warmed with 50ºC water bath (5.94 mM)
Water Insoluble
Ethanol Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。