A-779 (trifluoroacetate salt)

A-779 is a peptide antagonist of the Mas receptor, also known as the angiotensin (1-7) (Ang (1-7)) receptor (IC50 = 0.3 nM in a radioligand binding assay). It does not compete with angiotensin 1 (AT1) and AT2 receptor agonists for binding in adrenocortical membranes when used at a concentration of 1 µM and exhibits an IC50 value greater than 10 µM in adrenomedullary membranes. In vitro, A-779 inhibits Ang (1-7)-induced release of arachidonic acid from CHO cells transfected with Mas. A-779 (0.01 mg/kg) prevents the antidiuretic effects of Ang (1-7) in water-loaded rats. It also inhibits the Ang (1-7)-induced decrease in mean arterial pressure (MAP) when administered by microinjection into the nucleus of the solitary tract with no effect on basal MAP. A-779 increases urine flow rate and sodium excretion in male, but not female, rats when AT1 and AT2 receptors are blocked by the selective antagonists losartan (Cay-10006594) and PD 123319 (Cay-16099), respectively.Formal Name: 5-L-isoleucine-7-D-alanine-1-7-angiotensin II, trifluoroacetate salt. Molecular Formula: C39H60N12O11 . XCF3COOH. Formula Weight: 873.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 33 mg/ml, PBS (pH 7.2): 1 mg/ml. SMILES: O=C([C@H](CC1=CC=C(O)C=C1)NC([C@@H](NC([C@@H](NC([C@H](CC(O)=O)N)=O)CCCNC(N)=N)=O)C(C)C)=O)N[C@]([H])(C(N[C@@H](CC2=CNC=N2)C(N[C@@H](C(O)=O)C)=O)=O)[C@H](CC)C.FC(F)(C(O)=O)F. InChi Code: InChI=1S/C39H60N12O11.C2HF3O2/c1-6-20(4)31(37(60)49-28(15-23-17-43-18-45-23)34(57)46-21(5)38(61)62)51-35(58)27(14-22-9-11-24(52)12-10-22)48-36(59)30(19(2)3)50-33(56)26(8-7-13-44-39(41)42)47-32(55)25(40)16-29(53)54,3-2(4,5)1(6)7/h9-12,17-21,25-28,30-31,52H,6-8,13-16,40H2,1-5H3,(H,43,45)(H,46,57)(H,47,55)(H,48,59)(H,49,60)(H,50,56)(H,51,58)(H,53,54)(H,61,62)(H4,41,42,44),(H,6,7)/t20-,21+,25-,26-,27-,28-,30-,31-,/m0./s1. InChi Key: KEBJQEFOFJTHSC-VLIPIWRHSA-N.