Lu AF27139 - ≥99% , CAS No.2097117-06-9

CAS: 2097117-06-9 Cat. No.: L649989 分子式: C₂₁H₁₉ClF₃N₅O₂S 分子量: 497.92

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

概要

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.

Form:Solid

IC50& Target:P2X7

Specifications

仕様と純度

≥99%

生化学的・生理学的メカニズム

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

保管条件

Store at -20°C

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

ANTAGONIST

純度

≥99%

名前と識別子

• 分子量: 497.92

化学的性質と物理的性質

• 溶解度: DMSO : 125 mg/mL (251.04 mM; Need ultrasonic)

よくある質問

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

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.