[CAS NO. 2041075-86-7] Atuliflapon

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PRODUCTS SPECIFICATIONS [2041075-86-7]

Catalog

HY-122908

Brand

MCE

CAS

2041075-86-7

DESCRIPTION [2041075-86-7]

Overview

MDL	-
Molecular Weight	446.50
Molecular Formula	C24H26N6O3
SMILES	O=C([C@H]1[C@H](C(C2=CC=C(C3=NNC(C)=C3)C=C2)=O)CCCC1)NC4=C(N(N=C4)CCN5)C5=O

For research use only. We do not sell to patients.

Summary

Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein) , with an IC ₅₀ of 2 nM. Atuliflapon is used in the study for coronary artery disease ^[1] .

IC50 & Target

IC50: 2 nM (FLAP) ^[1] .

In Vitro

Atuliflapon demonstrates a dose dependent and greater than 90% suppression of leukotriene production over 24 h ^[1] .
Atuliflapon exhibits an IC ₅₀ of 39 nM for LTB ₄ ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04734275	AstraZeneca\|Parexel	Chronic Kidney Disease	February 1, 2021	Phase 1
NCT04492709	AstraZeneca\|Parexel	Cardiovascular Disease	July 30, 2020	Phase 1
NCT03400488	AstraZeneca	Coronary Artery Disease	January 16, 2018	Phase 1
NCT04492722	AstraZeneca\|Parexel\|George Clinical Pty Ltd	Chronic Kidney Disease	October 1, 2020	Phase 2
NCT04210388	AstraZeneca\|Parexel	Coronary Artery Disease (CAD)	January 14, 2020	Phase 1
NCT03317002	AstraZeneca	Coronary Artery Disease	October 30, 2017	Phase 2
NCT05251259	AstraZeneca	Asthma	January 27, 2022	Phase 2
NCT02963116	AstraZeneca	High Risk Coronary Artery Disease	December 20, 2016	Phase 1
NCT02632526	AstraZeneca	Healthy Male Subjects\|Cardiovascular Disease	February 10, 2016	Phase 1
NCT04601467	National University Heart Centre, Singapore\|AstraZeneca	Acute Coronary Syndrome	January 1, 2021	Phase 2
NCT03420092	AstraZeneca\|Parexel	Coronary Artery Disease	February 5, 2018	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 279.96 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2396 mL	11.1982 mL	22.3964 mL
5 mM	0.4479 mL	2.2396 mL	4.4793 mL
10 mM	0.2240 mL	1.1198 mL	2.2396 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[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.