AZD2716

• CAT Number: I047621
• CAS Number: 1845753-81-2
• Molecular Formula: C24H23NO3
• Molecular Weight: 373.44
• Purity: ≥95%
• IUPAC Name: (2R)-3-[3-(5-benzyl-2-carbamoylphenyl)phenyl]-2-methylpropanoic acid
• InChI: InChI=1S/C24H23NO3/c1-16(24(27)28)12-18-8-5-9-20(14-18)22-15-19(10-11-21(22)23(25)26)13-17-6-3-2-4-7-17/h2-11,14-16H,12-13H2,1H3,(H2,25,26)(H,27,28)/t16-/m1/s1
• SMILES: C[C@H](CC1=CC(=CC=C1)C2=C(C=CC(=C2)CC3=CC=CC=C3)C(=O)N)C(=O)O

AZD2716 is a novel, potent sPLA2 inhibitor (IC50 values of 10, 40, and 400 nM for sPLA2-IIa, -V, and -X, respectively) with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. When incubated with HepG2 cells, AZD2716 effectively inhibited sPLA2 activity (IC50 value of <14 nM) and suppressed production of sPLA2-IIa (IC50 value of 176 nM). AZD2716 also demonstrated significant sPLA2 activity inhibition (IC50 value of 56 nM) in atherosclerotic plaque homogenates. KEYWORDS: AZD2716 | supplier | sPLA2 inhibitor | AZD 2716 | AZD-2716 | CAS [1845753-81-2] | Phospholipids | PLA2 | Inhibitor | Enzymes | Coronary Artery Disease

Reference

F Giordanetto et al. Discovery of AZD2716: A Novel Secreted Phospholipase A2 (sPLA2) Inhibitor for the Treatment of Coronary Artery Disease. ACS Med Chem Lett. 2016 Aug 9;7(10):884-889.