[CAS NO. 306288-04-0] AVE0991sodiumsalt

Name: AVE0991sodiumsalt
Brand: Arctom Scientific
SKU: AS464252

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PRODUCTS SPECIFICATIONS [306288-04-0]

Fulfillment

Catalog

AS464252

Brand

Arctom Scientific

CAS

306288-04-0

DESCRIPTION [306288-04-0]

Overview

MDL	MFCD28167715
Molecular Weight	602.70
Molecular Formula	C29H31N4NaO5S2
SMILES	O=S(C1=C(C2=CC=C(CN3C(C=O)=C(OC)N=C3C4=CC=CC=C4)C=C2)C=C(CC(C)C)S1)([N-]C(NCC)=O)=O.[Na+]

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

10 Publications Citing Use of MCE

Summary

AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ ¹²⁵ I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC ₅₀ of 21 nM ^[1] .

IC50 & Target

IC50: 21±35 nM (Ang-(1-7) receptor) ^[1]

In Vitro

AVE 0991 is a nonpeptide compound that evokes effects similar to Ang-(1-7) on the endothelium. AVE 0991 and unlabeled Ang-(1-7) compete for high-affinity binding of [ ¹²⁵ I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC ₅₀ s of 21±35 and 220±280 nM, respectively. Peak concentrations of NO and O ₂ ^- release by AVE 0991 sodium salt and Ang-(1-7) (both 10 μM) are not significantly different (NO: 295±20 and 270±25 nM; O ₂ ^- : 18±2 and 20±4 nM). However, the released amount of bioactive NO is ≈5 times higher for AVE 0991 in comparison to Ang-(1-7) ^[1] .

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

In Vivo

AVE 0991 (0.58 nmol/g) produces a significant decrease of water diuresis in WT mice compared with vehicle-treated animals (0.06±0.03 mL versus 0.27±0.05; n=9 for each group; P<0.01). The antidiuretic effect of AVE 0991 (AVE) is associated with an increase in urine osmolality (1669±231.0 mOsm/KgH ₂ O versus 681.1±165.8 mOsm/KgH ₂ O in vehicle-treated mice; P<0.01). The genetic deletion of Mas abolishes the antidiuretic effect of AVE 0991 during water loading (0.37±0.10 mL [n=9] versus 0.27±0.03 mL [n=11] in AVE 0991-treated mice). As observed with C57BL/6 mice, administration of AVE 0991 (0.58 nmol/g) in water-loaded Swiss mice also produces a significant decrease of the urinary volume compared with vehicle-treated animals (0.13±0.05 mL [n=16] versus 0.51±0.04 mL [n=40]; P<0.01) ^[2] . One week of treatment with AVE-0991 produces a significant decrease in perfusion pressure (56.55±0.86 vs. 68.73±0.69 mmHg in vehicle-treated rats) and an increase in systolic tension (11.40±0.05 vs. 9.84±0.15 g in vehicle-treated rats), rate of tension rise (+dT/dt; 184.30±0.50 vs. 155.20±1.97 g/s in vehicle-treated rats), rate of tension fall (−dT/dt; 179.60±1.39 vs. 150.80±2.42 g/s in vehicle-treated rats). A slight increase in heart rate (HR) is also observed (220.40±0.71 vs. 214.20±0.74 beats/min in vehicle-treated rats ^[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

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 55 mg/mL ( 91.26 mM )

H ₂ O : 50 mg/mL ( 82.96 mM ; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6592 mL	8.2960 mL	16.5920 mL
5 mM	0.3318 mL	1.6592 mL	3.3184 mL
10 mM	0.1659 mL	0.8296 mL	1.6592 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.45 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.45 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.45 mM); Clear solution

* All of the co-solvents are available by MCE.