Atuliflapon

• CAT Number: I022879
• CAS Number: 2041075-86-7
• Molecular Formula: C24H26N6O3
• Molecular Weight: 446.50
• Purity: ≥95%
• Synonyms: (1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]-N-(4-oxo-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-3-yl)cyclohexane-1-carboxamide
• InChI: InChI=1S/C24H26N6O3/c1-14-12-19(29-28-14)15-6-8-16(9-7-15)22(31)17-4-2-3-5-18(17)23(32)27-20-13-26-30-11-10-25-24(33)21(20)30/h6-9,12-13,17-18H,2-5,10-11H2,1H3,(H,25,33)(H,27,32)(H,28,29)/t17-,18-/m1/s1
• InChIKey: ROTWSDMXHVGAHZ-QZTJIDSGSA-N
• SMILES: CC1=CC(=NN1)C2=CC=C(C=C2)C(=O)C3CCCCC3C(=O)NC4=C5C(=O)NCCN5N=C4

Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease[1].
Atuliflapon demonstrates a dose dependent and greater than 90% suppression of leukotriene production over 24 h[1].
Atuliflapon exhibits an IC50 of 39 nM for LTB4[1].
Atuliflapon exhibits t1/2 of 0.45 h and 2.1 h in rat and dog by iv injection, respectively[1].
Atuliflapon shows no inhibition of 5-LO pathway activity in rodent blood[1].

Reference

[1]. Daniel Pettersen, et al. Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease. J Med Chem. 2019 May 9;62(9):4312-4324.
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