Lu AF27139 - 10mM in DMSO , CAS No.2097117-06-9

CAS: 2097117-06-9 Cat. No.: L656086 Summenformel: C₂₁H₁₉ClF₃N₅O₂S Molekulargewicht: 497.92

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor ( IC 50 s of 12 and 2.4 nM for human and rat, K i s 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

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 IC 50 of 66 nM. Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose. Lu AF27139 (compound 1) inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC 50 of 38 ± 2.5 nM. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Lu AF27139 (compound 1) (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice . Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat . dose C u, plasma (nM) a C u, brain (nM) a C u, spinal cord (nM) a (mg/kg, po) (1 h) (2 h) (1 h) (2 h) (1 h) (2 h) T 1 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*f u ), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration and f u is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. f u , plasma = 0.02 ± 0.00, f u , spinal cord = 0.07 ± 0.03, and f u , brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague−Dawley rats (280−350 g); Male C57BL mice (18−25g) Dosage: 3, 10, and 100 mg/kg Administration: p.o. Result: Reduced intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.

IC50& Target:P2X7

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor ( IC 50 s of 12 and 2.4 nM for human and rat, K i s of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. L

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

ANTAGONIST

Namen und Kennungen

• Molekulargewicht: 497.92

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2097117-06-9, the molecular formula is C21H19ClF3N5O2S, and the molecular weight is 497.92 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.