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Zofenopril Calcium

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Chemical Structure| 81938-43-4 同义名 : SQ26991;Zofenopril (calcium salt)
CAS号 : 81938-43-4
货号 : A534063
分子式 : C44H44CaN2O8S4
纯度 : 98%
分子量 : 897.167
MDL号 : MFCD08704648
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(2.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Zofenopril calcium is an antioxidant and acts as an angiotensin-converting enzyme (ACE) inhibitor which has been shown to have beneficial effects in hypertension and heart failure. Zofenopril is also an inhibitor of PEPT2, the predominant peptide transporter in kidney and choroid plexus. Zofenopril is a pro-drug designed to undergo metabolic hydrolysis yielding the active free sulfhydryl compound zofenoprilat[3]. Zofenopril increases SR calcium cycling and stimulates active calcium uptake into the SR[4]. Administered orally 15 mg/kg for seven days, Zofenopril has been found effective in promoting nerve regeneration in sciatic nerve crush injury rat model[3]. As individual eliminating organs in dogs received a oral dose of zofenopril calcium (1.5 mg/kg), the gut and liver each had a high intrinsic capability to hydrolyze zofenopril; Extraction ratios (E) values ranged from 45 to 89%[5]. In dog model , Zofenopril was rapidly eliminated after parenteral administration; mean residence time values were 2 min and the elimination half-life values (intraarterial route only) were 9 min[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.11mL

0.22mL

0.11mL

5.57mL

1.11mL

0.56mL

11.15mL

2.23mL

1.11mL
参考文献

[1]Kalender AM, Dogan A, et al. Effect of Zofenopril on regeneration of sciatic nerve crush injury in a rat model. J Brachial Plex Peripher Nerve Inj. 2009 Jun 9;4:6.

[2]Dal Bo L, Mazzucchelli P, et al. Assay of zofenopril and its active metabolite zofenoprilat by liquid chromatography coupled with tandem mass spectrometry. J Chromatogr B Biomed Sci Appl. 2000 Dec 1;749(2):287-94.

[3]Kalender AM, Dogan A, Bakan V, Yildiz H, Gokalp MA, Kalender M. Effect of Zofenopril on regeneration of sciatic nerve crush injury in a rat model. J Brachial Plex Peripher Nerve Inj. 2009 Jun 9;4:6. doi: 10.1186/1749-7221-4-6. PMID: 19508704; PMCID: PMC2700796.

[4]Frascarelli S, Carnicelli V, Ghelardoni S, Chiellini G, Ronca F, Zucchi R. Effects of zofenopril on cardiac sarcoplasmic reticulum calcium handling. J Cardiovasc Pharmacol. 2009 Nov;54(5):456-63. doi: 10.1097/FJC.0b013e3181be7597. PMID: 19738489.

[5]Morrison RA, Burkett DE, Arnold ME, D'Arienzo CJ, Weinstein SH. Sites of first-pass bioactivation (hydrolysis) of orally administered zofenopril calcium in dogs. Pharm Res. 1991 Mar;8(3):370-5. doi: 10.1023/a:1015853801329. PMID: 2052527.