AVE 0991 sodium salt

Catalogue Number: B1213-APE

Manufacturer:	Apexbio
Type:	Biochemicals
Shipping Condition:	Blue Ice
Unit(s):	5 mg, 10 mg, 50 mg, 2 mg

Overview
Datasheets

Description

Description: IC50: AVE 0991 and Ang-(1-7) competitively bind to bovine aortic endothelial cell membranes with IC50 values of 21 +/- 35 and 220 +/- 280 nM, respectively.Angiotensin-(1-7) (Ang-[1-7]) acts as a crucial component of the renin-angiotensin system which can regulate and maintain the blood pressure by offsetting effects of Ang II, a typical vasoconstrictor in vivo. AVE 0991, a nonpeptide mimic of Ang-(1-7), performs as an agonist of angiotensin-(1-7) receptor. It plays an important role in exploring effects of Ang-(1-7) and evaluating the potential of Ang-(1-7) as a cardiovascular drug. [1]In vitro: AVE 0991 was found to compete with Ang-(1-7) for bovine aortic endothelial cell membrane receptors with an IC50 of 21+/-35 nM. There was no significant difference in peak concentrations of NO and O2- released from AVE 0991 treated group and Ang-(1-7) treated group. However, the released amount of NO was approximately 5 times higher in AVE 0991 group than that in Ang-(1-7) group. Moreover, AVE 0091 significantly displaced the binding of I-Ang-(1-7) in both Mas-transfected monkey kidney cells (COS) and Mas-transfected Chinese hamster ovary (CHO) cells. [1]In vivo: AVE 0091 at a dosage of 0.58 nmol/g resulted in a significant decrease in urinary volume, together with an increase in urinary osmolality in water-loaded C57BL/6 mice. [2] The antidiuretic effect of AVE was completely offset by the Ang II antagonists, which indicting a high specificity of AVE 0991. Since Ang II induced atherogenesis and ang-(1-7) offset Ang II action, it was proved that AVE 0991 blocked atherogenesis in apolipoprotein E (apoE)-knockout mice model. [3]Clinical trial: So far, no clinical trial has been conducted.References:[1]Wiemer G, Dobrucki LW, Louka FR, Malinski T, Heitsch H. AVE 0991, a nonpeptide mimic of the effects of angiotensin-(1-7) on the endothelium. Hypertension. 2002 Dec; 40: 847-52.[2] Pinheiro SV, Silva AC, Sampaio WO, Paula RD, Mendes EP, Bontempo ED, Pesquero JB, Walther T, Alenina N, Bader M, Bleich M and Santos RA. Nonpeptide AVE 0991 is an angiotensin-(1-7) receptor Mas agonist in the mouse kidney. Hypertension. 2004 Oct; 44(4):490-6.[3]Toton-Zuranska J, Gajda M, Pyka-Fosciak G, Kus K, Pawlowska M, Niepsuj A, Wolkow P, Olszanecki R, Jawien J and Korbut R. AVE 0991- angiotensin-(1-7) receptor agonist, inhibits atherogenesis in APOE-knockout mice. J Physiol Pharm. 2010, 61(2):181-183.

Additional Text

Storage Note

Store at -20°C

Short Description

Ang-(1-7) receptor Mas agonist

Solubility

Soluble in DMSO

Reagent:Smile String

CC/N=C([O-])/NS(C1=C(C2=CC=C(CN3C(C=O)=C(OC)N=C3C4=CC=CC=C4)C=C2)C=C(S1)CC(C)C)(=O)=O.[Na+]

B1213 Datasheet

B1213 CofA

B1213 MSDS

Price

£384.00

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