[CAS NO. 450348-85-3] AVE3085
PRODUCTS SPECIFICATIONS [450348-85-3]
DESCRIPTION [450348-85-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 317.29 |
| Molecular Formula | C17H13F2NO3 |
| SMILES | O=C(C1=CC=C(OC(F)(F)O2)C2=C1)NC3CC4=C(C=CC=C4)C3 |
Summary
AVE3085 is a potent endothelial nitric oxide synthase enhancer, used for cardiovascular disease treatment.
In Vitro
Pre-incubation with AVE3085 restores the bradykinin-induced relaxation, reverses the decrease of p-eNOS Ser1177 , and loares the level of p-eNOS Thr495 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 O 2 .− 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.
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.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 787.92 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.56 mM); Clear solution
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.
- [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
