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Lu AF27139

Catalog No. T9786   CAS 2097117-06-9

Lu AF27139 is an effective and selective 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 can be used in CNS diseases studies.

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Lu AF27139 Chemical Structure
Lu AF27139, CAS 2097117-06-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 93.00
5 mg In stock $ 228.00
10 mg In stock $ 378.00
25 mg In stock $ 639.00
50 mg In stock $ 913.00
100 mg In stock $ 1,230.00
500 mg In stock $ 2,490.00
1 mL * 10 mM (in DMSO) In stock $ 253.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lu AF27139 is an effective and selective 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 can be used in CNS diseases studies.
Targets&IC50 P2X7:12 nM (human), P2X7:2.4 nM (human), P2X7:22 nM (mouse), P2X7:54 nM (human)
In vitro Lu AF27139 (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose.
Lu AF27139 inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC50 of 38 ± 2.5 nM. Lu AF27139 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. Lu AF27139 (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].
In vivo In male Sprague−Dawley rats and male C57BL mice, Lu AF27139 (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex[1].
Molecular Weight 497.92
Formula C21H19ClF3N5O2S
CAS No. 2097117-06-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (241.00 mM), sonification is recommended.

TargetMolReferences and Literature

1. Hopper AT, et al. Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. J Med Chem. 2021;64(8):4891-4902.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library

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Keywords

Lu AF27139 2097117-06-9 Membrane transporter/Ion channel Neuroscience P2X Receptor Inhibitor P2XRs Lu AF-27139 oral P2X7 Lu AF 27139 rodent-active CNS-penetrant CNS inhibit inhibitor

 

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