Moexipril hydrochloride (Synonyms: RS-10085)

目录号: HY-B0378A 纯度: 98.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Moexipril hydrochloride (RS-10085) 是一种具有口服活性的血管紧张素转换酶 (ACE) 抑制剂，经水解为 moexiprilat 而发挥活性。Moexipril hydrochloride 具有降压和神经保护作用。

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Moexipril hydrochloride Chemical Structure

CAS No. : 82586-52-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥452	In-stock
10 mg	￥411	In-stock
25 mg	￥513	In-stock
50 mg	￥616	In-stock
100 mg	￥740	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

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Other Forms of Moexipril hydrochloride:

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生物活性
纯度 & 产品资料
参考文献

生物活性

Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril hydrochloride exhibits antihypertensive and neuroprotective effects^[1]^-^[4].

IC₅₀ & Target

IC50: 2.1 nM (purified ACE from rabbit lung), 1.75 nM (ACE in rat plasma)^[3]

体外研究
(In Vitro)

Moexipril hydrochloride is devoid of anti-inflammatory properties and has no effect on platelet function^[2].
Moexipril hydrochloride hydrolyzes to Moexiprilat, and Moexiprilat inhibits ACE in guinea pig serum as well as on purified ACE from rabbit lung with IC₅₀s of 2.6 and 4.9 nM, respectively^[2].
Moexipril hydrochloride (0.01 nM-0.1 mM) exhibits high potency against both plasma ACE and purified ACE from rabbit lung, with IC₅₀s of 2.7 mM and 0.165 mM, respectively^[3].
Moexipril hydrochloride (0-100 μM, 24 h) significantly reduced the percentage of damaged neurons in a dose-dependent manner^[4].
Moexipril hydrochloride (0-100 μM, 24 h) significantly attenuates Fe^2+/3+-induced neurotoxicity^[4].
Moexipril hydrochloride dose not cause significant changes in the percentage of apoptotic neurons^[4].

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

体内研究
(In Vivo)

Moexipril hydrochloride can not cross the blood-brain barrier^[1].
Moexipril hydrochloride (3 mg/kg, 30 mg/kg and 10 mg/kg, respectively; p.o.; once daily; 5 days) exhibits the a dose-dependent and antihypertensive effects in renal hypertensive rats, spontaneously hypertensive rats and perinephritic hypertensive dogs, respectively^[3].
Moexipril hydrochloride (0.3 mg/kg, i.p.) significantly reduces the infarct area on the mouse brain surface in NMRI mice^[4].
Moexipril hydrochloride (0.1 mg/kg, i.p.) significantly attenuates the cortical infarct volume in Long-Evans rats^[4].

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

Animal Model:	Spontaneously hypertensive rats^[3]
Dosage:	30 mg/kg
Administration:	Oral gavage; once daily; 5 days
Result:	Caused a progressive lowering of mean blood pressure from pretreatment values of 180 +/- 7 mmHg to a trough on day 4 of 127 +/- 4 mmHg. Dose-dependently decreased arterial blood pressure, and inhibited plasma and tissue ACE activity.

Animal Model:	Renal hypertensive rats^[3]
Dosage:	0.03-10 mg/kg
Administration:	Oral gavage; once daily; 5 days
Result:	Caused a dose-dependent decrease in blood pressure with a threshold dose of 0.3 mg/kg. Lowered mean blood pressure by about 70 mmHg of 3 mg/kg.

Animal Model:	Perinephritic hypertensive dogs^[3]
Dosage:	10 mg/kg
Administration:	Oral gavage; once daily; 5 days
Result:	Caused a drop of mean blood pressure by 25 mmHg from pre-treatment control, which persisted for 24 h, by a rapid onset and a long duration of action.

Animal Model:	NMRI mice (male, Permanent focal ischemia)^[4]
Dosage:	0, 0.03, 0.3, and 3 mg/kg
Administration:	Intraperitoneal injection (1 h before middle cerebral artery occlusion)
Result:	Significantly reduced the infarct area on the mouse brain surface with a dose of 0.3 mg/kg, and other doses were not effective.

Animal Model:	Long-Evans rats (male, Permanent focal ischemia)^[4]
Dosage:	0, 0.01, 0.1 mg/kg
Administration:	Intraperitoneal injection (1 h before middle cerebral artery occlusion)
Result:	Significantly attenuated the cortical infarct volume from 114.4 to 98.2 mm as compared to non-treated animals in a dose of 0.01 mg/kg, without reducing the infarct volume of the rat brain at dosages >0.01 mg/kg.

Clinical Trial

分子量

535.03

Formula

C₂₇H₃₅ClN₂O₇

CAS 号

82586-52-5

性状

固体

颜色

White to off-white

中文名称

盐酸莫西普利

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 250 mg/mL (467.26 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 100 mg/mL (186.91 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8691 mL	9.3453 mL	18.6905 mL
5 mM	0.3738 mL	1.8691 mL	3.7381 mL
10 mM	0.1869 mL	0.9345 mL	1.8691 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.89 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.89 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（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。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.89 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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。

方案一

请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (93.45 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 98.95%

选择批次：

Data Sheet (633 KB) SDS (398 KB)

COA (294 KB) LCMS (105 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Chrysant, S.G. and G.S. Chrysant, Pharmacological and clinical profile of moexipril: a concise review. J Clin Pharmacol, 2004. 44(8): p. 827-36. [Content Brief]

[2]. Friehe H, et al. Pharmacological and toxicological studies of the new angiotensin converting enzyme inhibitor moexipril hydrochloride. Arzneimittelforschung. 1997 Feb. 47(2):132-44. [Content Brief]

[3]. Edling, O., et al., Moexipril, a new angiotensin-converting enzyme (ACE) inhibitor: pharmacological characterization and comparison with enalapril. J Pharmacol Exp Ther, 1995. 275(2): p. 854-63. [Content Brief]

[4]. Ravati A, et al. Enalapril and moexipril protect from free radical-induced neuronal damage in vitro and reduce ischemic brain injury in mice and rats. Eur J Pharmacol. 1999 May 28;373(1):21-33. [Content Brief]

Moexipril hydrochloride 相关分类

Cardiovascular Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.8691 mL	9.3453 mL	18.6905 mL	46.7263 mL
	5 mM	0.3738 mL	1.8691 mL	3.7381 mL	9.3453 mL
	10 mM	0.1869 mL	0.9345 mL	1.8691 mL	4.6726 mL
	15 mM	0.1246 mL	0.6230 mL	1.2460 mL	3.1151 mL
	20 mM	0.0935 mL	0.4673 mL	0.9345 mL	2.3363 mL
	25 mM	0.0748 mL	0.3738 mL	0.7476 mL	1.8691 mL
	30 mM	0.0623 mL	0.3115 mL	0.6230 mL	1.5575 mL
	40 mM	0.0467 mL	0.2336 mL	0.4673 mL	1.1682 mL
	50 mM	0.0374 mL	0.1869 mL	0.3738 mL	0.9345 mL
	60 mM	0.0312 mL	0.1558 mL	0.3115 mL	0.7788 mL
	80 mM	0.0234 mL	0.1168 mL	0.2336 mL	0.5841 mL
	100 mM	0.0187 mL	0.0935 mL	0.1869 mL	0.4673 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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营业执照（三证合一）

Moexipril hydrochloride (Synonyms: RS-10085)

Other Forms of Moexipril hydrochloride: