| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 2 nM (FLAP). | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | Atuliflapon | ||||||||||||
| CAS | 2041075-86-7 | ||||||||||||
| Formula | C24H26N6O3 | ||||||||||||
| Molar Mass | 446.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |