Lu AF27139
Based on 1 Customer Validation
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.71%
- CAS No.: 2097117-06-9
- Formule: C21H19ClF3N5O2S
- Masse moléculaire:497.92
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Help & FAQs
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Activité biologique
Description
IC50 & Target
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P2X7 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Microglia | IC50 |
26 nM
Compound: 1; Lu AF27139
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Inhibition of BzATP-induced IL-1beta in mouse primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader
Inhibition of BzATP-induced IL-1beta in mouse primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader
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[PMID: 33822617] |
| Microglia | IC50 |
38 nM
Compound: 1; Lu AF27139
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Inhibition of BzATP-induced IL-1beta in rat primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader
Inhibition of BzATP-induced IL-1beta in rat primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader
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[PMID: 33822617] |
| THP-1 | IC50 |
38 nM
Compound: 1; Lu AF27139
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Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader
Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader
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[PMID: 33822617] |
In Vitro
Lu AF27139 (compound 1) (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC50 of 66 nM[1].
Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose[1].
Lu AF27139 (compound 1) inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC50 of 38 ± 2.5 nM[1].
Lu AF27139 (compound 1) concentration-dependently blocks IL-1β release in rat and mouse primary cortical microglia primed with LPS and induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat and 26 ± 6 nM in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat[1].
| dose | Cu, plasma (nM)a | Cu, brain (nM)a | Cu, spinal cord (nM)a | |||
| (mg/kg, po) | (1 h) | (2 h) | (1 h) | (2 h) | (1 h) | (2 h) |
| T1 | 22.4 ± 4.2 | 22.8 ± 10 | 5.4 ± 2.6 | 6.4 ± 2.0 | 5.20 ± 0.80 | 10.0 ± 2.0 |
a: Free plasma, brain, and spinal cord concentrations of Lu AF27139 in rat were determined by the formula (Ct*fu), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration and fu is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. fu, plasma = 0.02 ± 0.00, fu, spinal cord = 0.07 ± 0.03, and fu, brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague−Dawley rats (280−350 g); Male C57BL mice (18−25g)[1]
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Dosage:3, 10, and 100 mg/kg
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Administration:p.o.
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Result:Reduced intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.
Chemical Information
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CAS No. 2097117-06-9
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Appearance Solid
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Masse moléculaire 497.92
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Formule C21H19ClF3N5O2S
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Color White to off-white
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SMILES
ClC(C=C1)=CC=C1[C@H](N2CCOCC2)CNC(C3=C(C(F)(F)F)N=C(C4=NC=CC=N4)S3)=O
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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
In Vitro:
DMSO : 125 mg/mL (251.04 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)
In Vivo:
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 (4.18 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 (4.18 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.
In Vivo Dissolution Calculator
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 (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 |
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| DMSO | 1 mM | 2.0084 mL | 10.0418 mL | 20.0835 mL | 50.2089 mL |
| 5 mM | 0.4017 mL | 2.0084 mL | 4.0167 mL | 10.0418 mL | |
| 10 mM | 0.2008 mL | 1.0042 mL | 2.0084 mL | 5.0209 mL | |
| 15 mM | 0.1339 mL | 0.6695 mL | 1.3389 mL | 3.3473 mL | |
| 20 mM | 0.1004 mL | 0.5021 mL | 1.0042 mL | 2.5104 mL | |
| 25 mM | 0.0803 mL | 0.4017 mL | 0.8033 mL | 2.0084 mL | |
| 30 mM | 0.0669 mL | 0.3347 mL | 0.6695 mL | 1.6736 mL | |
| 40 mM | 0.0502 mL | 0.2510 mL | 0.5021 mL | 1.2552 mL | |
| 50 mM | 0.0402 mL | 0.2008 mL | 0.4017 mL | 1.0042 mL | |
| 60 mM | 0.0335 mL | 0.1674 mL | 0.3347 mL | 0.8368 mL | |
| 80 mM | 0.0251 mL | 0.1255 mL | 0.2510 mL | 0.6276 mL | |
| 100 mM | 0.0201 mL | 0.1004 mL | 0.2008 mL | 0.5021 mL |
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