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

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

For research use only. We do not sell to patients.

AVE3085 Chemical Structure

AVE3085 Chemical Structure

CAS No. : 450348-85-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 126 In-stock
Solution
10 mM * 1 mL in DMSO USD 126 In-stock
Solid
1 mg USD 90 In-stock
5 mg USD 180 In-stock
10 mg USD 290 In-stock
20 mg USD 460 In-stock
50 mg USD 920 In-stock
100 mg USD 1470 In-stock
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  • Biological Activity

  • Protocol

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Description

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-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].

MedChemExpress (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].

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

Molecular Weight

317.29

Formula

C17H13F2NO3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=C(OC(F)(F)O2)C2=C1)NC3CC4=C(C=CC=C4)C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (787.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

References
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.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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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AVE3085 Related Classifications

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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AVE3085
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