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  1. Metabolic Enzyme/Protease Apoptosis
  2. Angiotensin-converting Enzyme (ACE) Apoptosis
  3. Moexipril hydrochloride

Moexipril hydrochloride  (Synonyms: RS-10085)

目錄號(hào): HY-B0378A 純度: 98.95%
COA 產(chǎn)品使用指南 技術(shù)支持

Moexipril hydrochloride (RS-10085) 是一種具有口服活性的血管緊張素轉(zhuǎn)換酶 (ACE) 抑制劑,經(jīng)水解為 moexiprilat 而發(fā)揮活性。Moexipril hydrochloride 具有降壓和神經(jīng)保護(hù)作用。

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Moexipril hydrochloride Chemical Structure

Moexipril hydrochloride Chemical Structure

CAS No. : 82586-52-5

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10 mM * 1 mL in DMSO ¥452
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10 mg ¥411
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25 mg ¥513
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Other Forms of Moexipril hydrochloride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]

體外研究
(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 Fe2+/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.

體內(nèi)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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

鹽酸莫西普利

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 250 mg/mL (467.26 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

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

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.89 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.89 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。

以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑: PBS

    Solubility: 50 mg/mL (93.45 mM); 澄清溶液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 98.95%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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產(chǎn)品名稱:
Moexipril hydrochloride
目錄號(hào):
HY-B0378A
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