AVE-3085
目录号 : GC32486
AVE-3085是一种有效的nitricoxidesynthase增强剂，常用于治疗心血管疾病。
Cas No.:450348-85-3
Sample solution is provided at 25 µL, 10mM.
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AVE-3085 is a potent endothelial nitric oxide synthase enhancer, used for cardiovascular disease treatment.
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].
AVE 3085 (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 AVE 3085-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 AVE 3085 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].
[1]. Chen Y, et al. AVE 3085, a novel endothelial nitric oxide synthase enhancer, attenuates cardiac remodeling in mice through the Smad signaling pathway. Arch Biochem Biophys. 2015 Mar 15;570:8-13. [2]. Xue HM, et al. AVE3085 protects coronary endothelium from the impairment of asymmetric dimethylarginine by activation and recoupling of eNOS. Cardiovasc Drugs Ther. 2012 Oct;26(5):383-92. [3]. Yang Q, et al. AVE3085, an enhancer of endothelial nitric oxide synthase, restores endothelial function and reduces blood pressure in spontaneously hypertensive rats. Br J Pharmacol. 2011 Jul;163(5):1078-85
Animal experiment: | 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. |
References: [1]. Chen Y, et al. AVE 3085, a novel endothelial nitric oxide synthase enhancer, attenuates cardiac remodeling in mice through the Smad signaling pathway. Arch Biochem Biophys. 2015 Mar 15;570:8-13. | |
| Cas No. | 450348-85-3 | SDF | |
| Canonical SMILES | O=C(C1=CC=C(OC(F)(F)O2)C2=C1)NC3CC4=C(C=CC=C4)C3 | ||
| 分子式 | C17H13F2NO3 | 分子量 | 317.29 |
| 溶解度 | DMSO : 250 mg/mL (787.92 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 10 mM | 0.3152 mL | 1.5758 mL | 3.1517 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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