Art. -Nr.: HY-122908

Atuliflapon

(Synonyms: AZD5718)

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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.

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Reinheit: 98.65%
CAS. Nr.: 2041075-86-7
Formel: C₂₄H₂₆N₆O₃
Molecular Weight:446.50

Speicherung:

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

Atuliflapon Chemical Structure

CAS. Nr.: 2041075-86-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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].

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	2.3 μM Compound: 12; AZD5718	Substrate activity at recombinant human OATP1B1 expressed in HEK293 cells assessed as reduction in pivastatin uptake Substrate activity at recombinant human OATP1B1 expressed in HEK293 cells assessed as reduction in pivastatin uptake	[PMID: 30869888]
HepG2	IC₅₀	>250 μM Compound: 12; AZD5718	Cytotoxicity against human HepG2 cells assessed as reduction in ATP depletion in presence of glucose/galactose Cytotoxicity against human HepG2 cells assessed as reduction in ATP depletion in presence of glucose/galactose	[PMID: 30869888]
Sf21	IC₅₀	74 μM Compound: 12; AZD5718	Inhibition of recombinant human BSEP expressed in baculovirus infected Sf21 insect cell vesicles assessed as reduction in NBD-taurocholate uptake by fluorescence assay Inhibition of recombinant human BSEP expressed in baculovirus infected Sf21 insect cell vesicles assessed as reduction in NBD-taurocholate uptake by fluorescence assay	[PMID: 30869888]
Sf21	IC₅₀	74 μM Compound: 12; AZD5718	Inhibition of Sprague-Dawley rat Mrp2 expressed in baculovirus infected Sf21 insect cell vesicles assessed as reduction in CDF uptake by fluorescence assay Inhibition of Sprague-Dawley rat Mrp2 expressed in baculovirus infected Sf21 insect cell vesicles assessed as reduction in CDF uptake by fluorescence assay	[PMID: 30869888]
THP-1	IC₅₀	>250 μM Compound: 12; AZD5718	Cytotoxicity against human THP1 cells assessed as reduction in cell viability measured after 48 hrs by resazurin assay Cytotoxicity against human THP1 cells assessed as reduction in cell viability measured after 48 hrs by resazurin assay	[PMID: 30869888]

In Vitro

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].

MedChemExpress (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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2041075-86-7
Appearance Solid
Molecular Weight 446.50
Formel C₂₄H₂₆N₆O₃
Color White to off-white
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
Synonyms

AZD5718
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (279.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2396 mL	11.1982 mL	22.3964 mL	55.9910 mL
	5 mM	0.4479 mL	2.2396 mL	4.4793 mL	11.1982 mL
	10 mM	0.2240 mL	1.1198 mL	2.2396 mL	5.5991 mL
	15 mM	0.1493 mL	0.7465 mL	1.4931 mL	3.7327 mL
	20 mM	0.1120 mL	0.5599 mL	1.1198 mL	2.7996 mL
	25 mM	0.0896 mL	0.4479 mL	0.8959 mL	2.2396 mL
	30 mM	0.0747 mL	0.3733 mL	0.7465 mL	1.8664 mL
	40 mM	0.0560 mL	0.2800 mL	0.5599 mL	1.3998 mL
	50 mM	0.0448 mL	0.2240 mL	0.4479 mL	1.1198 mL
	60 mM	0.0373 mL	0.1866 mL	0.3733 mL	0.9332 mL
	80 mM	0.0280 mL	0.1400 mL	0.2800 mL	0.6999 mL
	100 mM	0.0224 mL	0.1120 mL	0.2240 mL	0.5599 mL

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Atuliflapon

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Atuliflapon

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Atuliflapon Related Classifications

HY-122908 Related Classifications