Trandolapril|87679-37-6|(群多普利; RU44570)-陌孚医药/Medlife

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Trandolapril (Synonyms: 群多普利; RU44570)

目录号: PC15726 纯度: ≥98%

CAS No. :87679-37-6

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中文名称

Trandolapril

中文别名

群多普利;(2S,3aR,7aS)-1-[(2S)-2-[[(1S)-1-乙氧基甲酰-3-苯基-丙基]氨基]丙酰基]-2,3,3a,4,5,6,7,7a-八氢吲哚-2-甲酸;群多普利 EP标准品;群多普利 USP标准品;群多普利、;群多普利-D5;(3ΑR.7ΑS)-1-[N-[1(S)-乙氧羰基]-3-苯丙基]-(S)-丙氨酰八氢吲哚-2(S)-羧酸;泉多普利

英文名称

Trandolapril

英文别名

Trandolapril;(2s,3ar,7as)-1-[(2s)-2-[[(1s)-1-ethoxycarbonyl-3-phenyl-propyl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid;(2S,3aR,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid;RU44570;(2S,3aR,7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylic acid;(2S,3aR,7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylic acid,form I crystalline polymorph of;1-[2-[(1-ethoxycarbonyl-3-phenylpropyl)amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid;Odrik;Preran;Trandolaprilum [Latin];Mavik

Cas No.

87679-37-6

分子式

C₂₄H₃₄N₂O₅

分子量

430.54

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Trandolapril (RU44570) is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).

性状

Solid

IC50 & Target[1][2]

Target: Angiotensin-converting Enzyme (ACE)

体外研究(In Vitro)

Trandolapril (0.02 mM, 1 mM; 3 d) inhibits cell growth and induces cell apoptosis, increases the percentage of apoptotic cells in K562 cell line.

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

Apoptosis Analysis

Cell Line:	K562, KU812, U937 and HL60
Concentration:	0-2 mM
Incubation Time:	0, 1, 2, 3 days
Result:	Inhibited K562, KU812, U937 at 1 mM and inhibited HL60 at 0.02 mM.

体内研究(In Vivo)

Trandolapril (3 mg/kg/day; p.o.; 7 d) reduces renal fibrosis in obstructive nephropathy in mice, by inhibiting renal interstitial matrix expression and myofibroblast activation, decreasing renal proinflammatory cytokine RANTES and TNF-α level.
Trandolapril (0.3 mg/kg/day; p.o.; 4 weeks) improves arterial mechanics in rats, prevents arterial hypertrophy, collagen and cellular fibronectin accumulation.
randolapril (0.3 mg/kg/day; p.o.; 4 months) exhibits a chronic anti-hypertension effects in rats, results in blood pressure decreasing.
Trandolapril (0.25 mg/kg; p.o.; twice a day; 4 months) inhibits Atherosclerosis in the Watanabe Heritable Hyperlipidemic Rabbit.

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

Animal Model:	UUD (unilateral ureteral obstruction) model in Male CD-1 mice (18-22 g)
Dosage:	3 mg/kg
Administration:	Oral gavage; daily, for 7 days
Result:	Resulted in renal interstitial matrix expression (including fibronectin, type I, and type III collagen) decreasing, and inhibited myofibroblast activation by surprising a-smooth muscle actin (a-SMA) expression, decreased the RANTES (regulated on activation, normal T cell expressed and secreted) and TNF-α level.

Animal Model:	SHR model (spontaneously hypertensive rats, 4-week-old)
Dosage:	0.3 mg/kg
Administration:	Oral gavage; daily for 4 weeks
Result:	Reduced collagen content in the aortic media and increased ariterial distensibility up to about 80%.

Animal Model:	Watanabe heritable hyperlipidemic rabbit (3 months old)
Dosage:	0.25 mg/kg
Administration:	Oral gavage; twice a day; 9 months
Result:	Decreased in atherosclerotic involvement of the intimal surface, and also decreased cholesterol content in descending thoracic aorta.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Peters DC, et al. Trandolapril. An update of its pharmacology and therapeutic use in cardiovascular disorders. Drugs. 1998 Nov;56(5):871-93. [Information]

[2]. Tan X, et al. Combination therapy with paricalcitol and trandolapril reduces renal fibrosis in obstructive nephropathy. Kidney Int. 2009 Dec;76(12):1248-57. [Information]

[3]. Koffi I, et al. Prevention of arterial structural alterations with verapamil and trandolapril and consequences for mechanical properties in spontaneously hypertensive rats. Eur J Pharmacol. 1998 Nov 13;361(1):51-60. [Information]

[4]. Chobanian AV, et al. Trandolapril inhibits atherosclerosis in the Watanabe heritable hyperlipidemic rabbit. Hypertension. 1992 Oct;20(4):473-7. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (232.27 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	2.3227 mL	11.6133 mL	23.2266 mL
5 mM	0.4645 mL	2.3227 mL	4.6453 mL
10 mM	0.2323 mL	1.1613 mL	2.3227 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。-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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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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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