1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Olmesartan medoxomil

Olmesartan medoxomil  (Synonyms: 奥美沙坦酯; CS 866)

目录号: HY-17005 纯度: 99.67%
COA 产品使用指南

Olmesartan medoxomil 是一种有效的选择性的 血管紧张素 (angiotensin AT1) 受体抑制剂,IC50 为 66.2 μM。

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Olmesartan medoxomil Chemical Structure

Olmesartan medoxomil Chemical Structure

CAS No. : 144689-63-4

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10 mM * 1 mL in DMSO ¥610
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5 mg ¥343
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10 mg ¥550
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50 mg ¥700
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500 mg ¥3450
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Customer Review

Other Forms of Olmesartan medoxomil:

查看 Angiotensin Receptor 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.

IC50 & Target

AT1 Receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Vero C1008 EC50
> 40 μM
Compound: Olmesartan
Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
10.1101/2020.04.03.023846
体外研究
(In Vitro)

Inhibition of Arachidonic acid (AA) metabolism by angiotensin II receptor blockers (ARBs) is detected in a concentration-dependent manner with IC50 of Olmesartan (66.2 μM)[1]. Olmesartan medoxomil (OLM) is a potent and selective angiotensin AT1 receptor blocker[2].

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

体内研究
(In Vivo)

The efficacy of Olmesartan (20 mg/kg) studied in db/db diabetic mice for a period of 12 weeks starting from week 10 to 12 of age. The db/db mice have 11.7 fold increased albuminuria in comparison to control mice at week 22 to 24 of age. Twelve weeks Olmesartan administration significantly reduces albuminuria in db/db mice by 77% as compared with placebo treated db/db mice. The albumin/creatinine ratio (ACR) is increased in db/db mice in comparison to control mice by 7.1 fold and Olmesartan treatment significantly decreases ACR by 59% in db/db mice[3].

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

分子量

558.59

Formula

C29H30N6O6

CAS 号
性状

固体

颜色

White to yellow

中文名称

奥美沙坦酯

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (89.51 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)

Ethanol 中的溶解度 : 12.5 mg/mL (22.38 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 1.7902 mL 8.9511 mL 17.9022 mL
5 mM 0.3580 mL 1.7902 mL 3.5804 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

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 (3.72 mM); 澄清溶液; 超声助溶

    此方案可获得 2.08 mg/mL的澄清溶液。

    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 (3.72 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。

    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。

    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。
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)。
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

纯度: 99.67%

参考文献
Animal Administration
[3]

Mice[3]
10 to 12-week old male db/db diabetic mice with background strain C57BL/KsJ and their age-matched non-diabetic lean control mice (C57BL) are used.10 non-diabetic control mice and 10 diabetic mice are fed with placebo (0.5% sodium CMC/saline solution), and 10 diabetic mice are fed with 20 mg/kg Olmesartan (MB5704) by daily gavage for 12 weeks. Mice are monitored for blood glucose, body weight and urine output every two weeks. After treatment, mice are euthanized and trunk blood is collected and is centrifuged to obtain plasma which is aliquoted and stored at -80°C. Kidney tissues are removed from mice. For protein extraction slices of the kidney tissue are frozen in liquid nitrogen, and stored at -80°C. Other parts of the kidney tissue are fixed with 4% paraformaldehyde and embedded in paraffin for immunostaining.

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.7902 mL 8.9511 mL 17.9022 mL 44.7555 mL
5 mM 0.3580 mL 1.7902 mL 3.5804 mL 8.9511 mL
10 mM 0.1790 mL 0.8951 mL 1.7902 mL 4.4756 mL
15 mM 0.1193 mL 0.5967 mL 1.1935 mL 2.9837 mL
20 mM 0.0895 mL 0.4476 mL 0.8951 mL 2.2378 mL
DMSO 25 mM 0.0716 mL 0.3580 mL 0.7161 mL 1.7902 mL
30 mM 0.0597 mL 0.2984 mL 0.5967 mL 1.4919 mL
40 mM 0.0448 mL 0.2238 mL 0.4476 mL 1.1189 mL
50 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
60 mM 0.0298 mL 0.1492 mL 0.2984 mL 0.7459 mL
80 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5594 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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产品名称:
Olmesartan medoxomil
目录号:
HY-17005
需求量: