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Captopril

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Chemical Structure| 62571-86-2 同义名 : 甲巯丙脯酸 ;SQ 14225;SA 333;Captopril, Capoten, SQ14225, SQ 14225, SQ-14225, SQ14,225, SQ 14,225, SQ-14,225
CAS号 : 62571-86-2
货号 : A177871
分子式 : C9H15NO3S
纯度 : 99%
分子量 : 217.285
MDL号 : -
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(230.11 mM)，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

H2O: 50 mg/mL(230.11 mM)
动物实验配方：
生物活性
靶点

  • ACE

    ACE, IC50:6 nM
描述 Angiotensin-converting enzyme (ACE) is helpful in controling blood pressure and converting the hormone angiotensin I to be active. Captopril is an ACE inhibitor with IC50 of 6 nM which can reduce the risk of doubling the serum creatinine concentration by almost 50% in patients and also be helpful in renal dysfunction therapy and blood pressure reduction. Besides, Captopril can also be used for the treatment of diabetic nephropathy and left ventricular dysfunction. This drug can reach to peak hypotensive effect in 1 - 1.5 hrs with about 30% protein binding ratio and serum half-life of 2 hrs[1]. LNM35 cells treated with captopril of concentrations from 0.01 to 10 mM for 24 hrs showed inhibitory impact on the cell viability at all these concentrations, the differences were significant in the concentrations of 0.1, 1 and 10 mM. While LNM35 cells treated with captopril of concentrations from 0.001 to 10 mM in FBS buffer for 24 - 48 hrs demonstrated induction of cell apoptosis from 2.5% for control group to 9% and 15.5% for captopril-treated cells, respectively. The higher of the captopril concentrations, the more of the apoptosis induction. NMRI female nude mice with about 100 mm3 tumors were treated with 2.8 mg captopril per mouse and the results showed that the human tumor xenografts growth was significantly reduced by 52% and 58% at the 18 and 21 days respectively. Furthermore, the mean lymph node weight was 63.5 mg in the captopril-treated group, smaller than that in the control group (127mg). Captopril also decreased the tumor cell proliferation by assessing the levels of the nuclear antigen Ki-67 in Ki-67-positive cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.60mL

0.92mL

0.46mL

23.01mL

4.60mL

2.30mL

46.02mL

9.20mL

4.60mL
参考文献

[1]Zaman MA, Oparil S, et al. Drugs targeting the renin-angiotensin-aldosterone system. Nat Rev Drug Discov. 2002;1(8):621-36.

[2]Attoub S, Gaben AM, et al. Captopril as a potential inhibitor of lung tumor growth and metastasis. Ann N Y Acad Sci. 2008.

[3]Kanda T, Inoue M, et al. Low-dose combination therapy with metoprolol and captopril for congestive heart failure in mice. Cardiovasc Drugs Ther. 1993 Nov;7(5):795-800.

[4]Larivière R, Lebel M, et al. Effects of losartan and captopril on endothelin-1 production in blood vessels and glomeruli of rats with reduced renal mass. Am J Hypertens. 1998 Aug;11(8 Pt 1):989-97.

[5]Antonaccio MJ, Rubin B, et al. Effects of captopril on vascular reactivity of SHR in vivo and in vitro. Hypertension. 1981 Nov-Dec;3(6 Pt 2):II-211-5.

[6]Boskabadi J, Mokhtari-Zaer A, et al. The effect of captopril on lipopolysaccharide-induced lung inflammation. Exp Lung Res. 2018 May - Jun;44(4-5):191-200.

[7]Siska S, Mun Im A, et al. Effect of Apium graveolens Extract Administration on the Pharmacokinetics of Captopril in the Plasma of Rats. Sci Pharm. 2018 Feb 16;86(1). pii: E6.