Atuliflapon
Based on 1 Customer Validation
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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- Pureté: 98.97%
- CAS No.: 2041075-86-7
- Formule: C24H26N6O3
- Masse moléculaire:446.50
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Activité biologique
IC50: 2 nM (FLAP)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2.3 μM
Compound: 12; AZD5718
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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
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[PMID: 30869888] |
| HepG2 | IC50 |
>250 μM
Compound: 12; AZD5718
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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
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[PMID: 30869888] |
| Sf21 | IC50 |
74 μM
Compound: 12; AZD5718
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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
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[PMID: 30869888] |
| Sf21 | IC50 |
74 μM
Compound: 12; AZD5718
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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
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[PMID: 30869888] |
| THP-1 | IC50 |
>250 μM
Compound: 12; AZD5718
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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
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[PMID: 30869888] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2041075-86-7
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Appearance Solid
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Masse moléculaire 446.50
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Formule C24H26N6O3
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Color White to off-white
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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
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Synonyms
AZD5718
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
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.
| 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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