1. Metabolic Enzyme/Protease
  2. Angiotensin-converting Enzyme (ACE)
  3. Omapatrilat

Omapatrilat  (Synonyms: BMS-186716)

目录号: HY-18208 纯度: 99.88%
COA 产品使用指南

Omapatrilat是金属蛋白酶ACENEP的双重抑制剂,Ki值分别为0.64和0.45 nM。

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Omapatrilat Chemical Structure

Omapatrilat Chemical Structure

CAS No. : 167305-00-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥902
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5 mg ¥820
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10 mg ¥1450
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25 mg ¥3100
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50 mg ¥5580
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100 mg ¥9980
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500 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.

IC50 & Target

Ki: 0.45 nM (NEP), 0.64 nM (ACE)[1]; IC50: 8 nM (NEP), 5 nM (ACE)[2]

体外研究
(In Vitro)

Omapatrilat exhibits high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (Ki=0.45, 25, 0.64, 250 nM) [1]. In vitro autoradiography using the specific NEP inhibitor radioligand 125I-RB104 and the specific ACE inhibitor radioligand 125I-MK351A show omapatril at (10 mg/kg) causes rapid and potent inhibition of renal NEP and ACE, respectively, for 24 h[4].

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

体内研究
(In Vivo)

Omapatrilat demonstrates excellent blood pressure lowering in a variety of animal models characterized by various levels of plasma renin activity and significantly potentiates urinary sodium, ANP, and cGMP excretion in a cynomolgus monkey assay. Omapatrilat decreases mean arterial pressure (MAP) approximately 40 mmHg below baseline from 10 to 24 h. Oral administration of omapatrilat at 100 μM/kg once daily results in a 38 mmHg decrease in systolic blood pressure at day three as compared to vehicle [2]. Omapatrilat is widely used in experimental protocols related to hypertension and heart failure. Chronic oral administration of omapatrilat reduces aortic leakiness and atheroma formation with enhanced endothelial independent vasorelaxation to ANP[3]. Omapatrilat causes significant inhibition of plasma ACE and increased plasma renin activity in rats[4].

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

分子量

408.53

Formula

C19H24N2O4S2

CAS 号
性状

固体

颜色

White to gray

中文名称

奥马曲拉

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 31 mg/mL (75.88 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4478 mL 12.2390 mL 24.4780 mL
5 mM 0.4896 mL 2.4478 mL 4.8956 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 (protect from light, stored under nitrogen)。-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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

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: ≥ 4.25 mg/mL (10.40 mM); 澄清溶液

    此方案可获得 ≥ 4.25 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 42.5 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.12 mM); 澄清溶液

    此方案可获得 ≥ 2.5 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。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

Omapatrilat is dissolved in 100% DMSO at 10 mM and diluted to 1% DMSO. NEP, NEP2, ACE and APP assays are performed at pH 7.4. The reaction buffer for NEP and NEP2 contained 50 mM HEPES, 140 mM NaCl, 10 mM KCl, 0.01% BSA. The buffer for ACE contained 100 mM Tris-HCl, 50 mM NaCl, 10 μM ZnCl2, and the buffer for APP contained 100 mM HEPES and 0.01% BSA. Assays are performed in 100 μL volume in black 96-well round-bottom plates at room temperature. Reactions are continuously monitored with excitation and emission wavelengths appropriate for each respective substrate. Enzyme velocity is determined from the linear part of the reaction[1].

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

Animal Administration
[3][4]

Rats: Sprague Dawley rats are weighed and then gavaged with vehicle (5% arabic gum) or omapatrilat (0.1, 1, 10 mg/kg) (n 5 6 rats/group). Rats are killed by decapitation at 1 h after gavage. Trunk blood is collected into prechilled tubes containing EDTA/aprotinin for the measurement of PRA and into prechilled heparin tubes for the measurement ofplasma ACE[4].

Rabbits: Omapatrilat is dissolved in drinking water. Rabbits are divided into 2 groups with 1% cholesterol diet, placebo-treated group and omapatrilat-treated group, and administrated (12 mg/Kg/day omapatrilat) once daily for 8 weeks. To demonstrate the acute effect of omapatrilat, urine is collected after omapatrilat or placebo administration for 24 hours at day 1, and urine volume, cGMP and ANP levels are assessed[3].

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

参考文献

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 (protect from light, stored under nitrogen)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4478 mL 12.2390 mL 24.4780 mL 61.1950 mL
5 mM 0.4896 mL 2.4478 mL 4.8956 mL 12.2390 mL
10 mM 0.2448 mL 1.2239 mL 2.4478 mL 6.1195 mL
15 mM 0.1632 mL 0.8159 mL 1.6319 mL 4.0797 mL
20 mM 0.1224 mL 0.6120 mL 1.2239 mL 3.0598 mL
25 mM 0.0979 mL 0.4896 mL 0.9791 mL 2.4478 mL
30 mM 0.0816 mL 0.4080 mL 0.8159 mL 2.0398 mL
40 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5299 mL
50 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2239 mL
60 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0199 mL
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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