1. Immunology/Inflammation
  2. NO Synthase
  3. AVE3085

AVE3085 是一种有效的 nitric oxide synthase 增强剂,常用于心血管疾病的研究。

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AVE3085 Chemical Structure

AVE3085 Chemical Structure

CAS No. : 450348-85-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1256
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1 mg ¥900
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5 mg ¥1800
In-stock
10 mg ¥2900
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20 mg ¥4600
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100 mg   询价  
200 mg   询价  

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查看 NO Synthase 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

AVE3085 is a potent endothelial nitric oxide synthase enhancer, used for cardiovascular disease treatment.

体外研究
(In Vitro)

Pre-incubation with AVE3085 restores the bradykinin-induced relaxation, reverses the decrease of p-eNOSSer1177, and loares the level of p-eNOSThr495 and nitrotyrosine. NO release in response to bradykinin is significantly reduced by ADMA and such reduction is restored by AVE3085. AVE3085 also prevents the elevation of O2.− and ONOO levels in coronary arteries exposed to ADMA[2]. AVE3085 (10 μM) markedly increases ACh-induced relaxations in SHR aortae without affecting those in WKY aortae, and also increases the eNOS expression in WKY aortae[3].

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

体内研究
(In Vivo)

AVE3085 (10 mg/kg/day, p.o.) treatment prevents the increases in the left ventricular weight, left ventricular weight/body weight ratio, mean myocyte diameter, and the expression of the hypertrophic markers ANP and β-MHC compared to the vehicle-treated mice. AVE 3085 treatment also attenuates the collagen volume fraction levels compared to the vehicle-treated mice. In the AVE3085-treated mice, the EFs, FSs, mitral E velocity, E/A ratio and LVDds are significantly improved compared to the vehicle-treated mice. AVE 3085 treatment attenuates the increase in the expression of Smad2 mRNA. Furthermore, the levels of the eNOS protein expression are significantly up-regulated in the AVE3085 group than in the vehicle-treated AB group[1]. AVE3085 (10 mg/kg, p.o.) significantly improves ACh-induced endothelium-dependent relaxations in the aortae of SHRs, and reduces systolic blood pressure in SHRs. AVE3085 treatment for 4 weeks increases levels of p-eNOS and eNOS in SHR aortae without affecting levels of eNOS and p-eNOS in WKY aortae[3].

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

分子量

317.29

Formula

C17H13F2NO3

CAS 号
性状

固体

颜色

White to light yellow

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 : 250 mg/mL (787.92 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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1517 mL 15.7585 mL 31.5169 mL
5 mM 0.6303 mL 3.1517 mL 6.3034 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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.56 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。

    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。

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: 99.95%

参考文献
Animal Administration
[1]

Male C57BL/6J mice (8-10 weeks old; 24-26 g) are housed in individual cages on a 12 h light-dark cycle in a temperature- (24 ± 2°C) and humidity-controlled room with ad libitum access to tap water and standard rodent chow. The mice are anesthetized via an intraperitoneal injection of 1.5% pentobarbital (W*0.06), and cardiac hypertrophy is induced by pressure overload, which is achieved via descending aortic banding (AB). Similar surgeries that do not include aortic banding are performed on the sham-operated. Twenty-four hours after ligation, the surviving mice are randomly divided into the following three groups (n=8 per group): (1) a sham-operated group (Sham group), (2) a vehicle-treated AB group (vehicle-treated group), and (3) an AB group treated with AVE 3085 (AVE 3085 group). AVE 3085 is administered orally once daily at a dose of 10 mg kg day−1 for 4 weeks, and isovolumic sodium chloride is administered in the same manner to the sham-operated and vehicle-treated groups.

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
DMSO 1 mM 3.1517 mL 15.7585 mL 31.5169 mL 78.7923 mL
5 mM 0.6303 mL 3.1517 mL 6.3034 mL 15.7585 mL
10 mM 0.3152 mL 1.5758 mL 3.1517 mL 7.8792 mL
15 mM 0.2101 mL 1.0506 mL 2.1011 mL 5.2528 mL
20 mM 0.1576 mL 0.7879 mL 1.5758 mL 3.9396 mL
25 mM 0.1261 mL 0.6303 mL 1.2607 mL 3.1517 mL
30 mM 0.1051 mL 0.5253 mL 1.0506 mL 2.6264 mL
40 mM 0.0788 mL 0.3940 mL 0.7879 mL 1.9698 mL
50 mM 0.0630 mL 0.3152 mL 0.6303 mL 1.5758 mL
60 mM 0.0525 mL 0.2626 mL 0.5253 mL 1.3132 mL
80 mM 0.0394 mL 0.1970 mL 0.3940 mL 0.9849 mL
100 mM 0.0315 mL 0.1576 mL 0.3152 mL 0.7879 mL
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  • 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:
AVE3085
目录号:
HY-19504
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