Fosinopril sodium|88889-14-9|(福辛普利钠; SQ28555)-陌孚医药/Medlife

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Fosinopril sodium (Synonyms: 福辛普利钠; SQ28555)

目录号: PC15671 纯度: ≥98%

CAS No. :88889-14-9

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中文名称	Fosinopril sodium
中文别名	福辛普利钠;4-环己基-1-[(2-甲基-1-(丙酰氧基)丙氧基)(4-苯基丁基)膦酰乙酰基]-L-脯氨酸钠;福辛普利-D7钠盐;福辛普利钠 EP标准品;福辛普利钠 USP标准品;福辛普利钠盐;蒙诺(福辛普利那)
英文名称	Fosinopril sodium
英文别名	Fosinopril sodium;(4S)-4-Cyclohexyl-1-{[(RS)-2-methyl-1-(propionyloxy)propoxy]-(4-phenylbutyl)phosphinylacetyl}-L-proline sodium salt;Fosinopril SodiuM Salt;Sodium (2S,4S)-4-cyclohexyl-1-(2-((2-methyl-1-(propionyloxy)propoxy)-(4-phenylbutyl)phosphoryl)acetyl)pyrrolidine-2-car...;Sodium (2S,4S)-4-cyclohexyl-1-(2-((2-methyl-1-(propionyloxy)propoxy)-(4-phenylbutyl)phosphoryl)acetyl)pyrrolidine-2-carboxylate;sodium,(2S,4S)-4-cyclohexyl-1-[2-[(2-methyl-1-propanoyloxypropoxy)-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylate;(2S,4S)-4-Cyclohexyl-1-(2-{[2-methyl-1-(propanoyloxy)propoxy](4-phenylbutyl)phosphoryl}acetyl)pyrrolidine-2-carboxylic acid;Acecor;Eosinopril;Fosinopril;Monopril;SQ 28555;Secorvas;Staril;C30H45NNaO7P;Fosinopril sodium [USAN];Sodium (2S,4S)-4-cyclohexyl-1-(2-((2-methyl-1-(propionyloxy)propoxy)(4-phenylbutyl)phosphoryl)acetyl)pyrrolidine-2-carboxylate;Tensogard;Hiperlex;Fosipres;Dynacil;Fosinorm;Fosinil;Foziretic;Fositens;Fositen;Eliten;Sapril;Newace;Tenso Stop;Acenor-M;FOSINOPRIL?SODIUM;DSSTox_CID_26621;DSSTox_RID_81772;DSSTox_GSID_46621
Cas No.	88889-14-9
分子式	C₃₀H₄₅NNaO₇P
分子量	585.64
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.

性状

Solid

IC50 & Target[1][2]

IC₅₀: 0.18 μM; Ki: 1.675 μM

体外研究(In Vitro)

Fosinopril (0, 1, 10, 33, 100μM; 30 min) partially inhibits the cosedimentation of liposomes and recombinant LPLA2.
Fosinopril (250 nM) shows no inhibition of the soluble esterase activity of LPLA2.
Fosinopril (0.372, 0.744, 1.116 μM) displays a non-competitive inhibition effect on ACE activity with a K_i value of 1.675 μM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Fosinopril (orally; 4.67 mg/kg; 4 weeks) downregulates the creatine kinase (CK) and lactate dehydrogenase (LDH) levels and against cardiac dysfunction and structural alteration.
Fosinopril (orally; 4.67 mg/kg; 4 weeks) suppresses cleaved-caspase 3 expression and myocardial apoptosis in AMI rat model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	HF post-acute myocardial infarction (AMI) rat model (SPF-grade Sprague-Dawley (SD) rats, 265 ± 15 g)
Dosage:	4.67 mg/kg
Administration:	p.o.; 4 weeks
Result:	Against cardiac dysfunction and structural alteration and suppressed apoptosis.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

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

ClinicalTrial

参考文献

[1]. Ondetti, M.A., Structural relationships of angiotensin converting-enzyme inhibitors to pharmacologic activity. Circulation, 1988. 77(6 Pt 2): p. I74-8. [Information]

[2]. Piepho, R.W., Overview of the angiotensin-converting-enzyme inhibitors. Am J Health Syst Pharm, 2000. 57 Suppl 1: p. S3-7. [Information]

[3]. Sharma, S., et al., The hemodynamic effects of long-term ACE inhibition with fosinopril in patients with heart failure. Fosinopril Hemodynamics Study Group. Am J Ther, 1999. 6(4): p. 181-9. [Information]

溶解度数据

体外研究:

H₂O : 33.33 mg/mL (56.91 mM; Need ultrasonic)

Ethanol : 16.67 mg/mL (28.46 mM; Need ultrasonic)

DMSO : 1.43 mg/mL (2.44 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7075 mL	8.5377 mL	17.0753 mL
5 mM	0.3415 mL	1.7075 mL	3.4151 mL
10 mM	0.1708 mL	0.8538 mL	1.7075 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 9.09 mg/mL (15.52 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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