YM-90709

SKU: orb1226010

Description

A potent IL-5 receptor antagonist that inhibits the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells with IC50 of 1.0 and 0.57 uM, respectively; inhibits IL-5-prolonged eosinophil survival with IC50 of 0.45 uM and does not affect the GM-CSF-prolonged eosinophil survival; inhibits antigen-induced infiltration of eosinophils and lymphocytes into the bronchoalveolar lavage fluid (BALF) in BN rats (EC50=0.32 mg/kg and 0.12 mg/kg, respectively).

Key Properties

• CAS Number: 163769-88-8
• MW: 359.4211
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₁N₃O₂
• SMILES: CC(CC1=CC(OC)=C(OC)C=C12)(C)N3C2=CC4=NC5=CC=CC=C5N=C43
• Target: IL Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  YM-90709 (0.01-10 mg/kg; intravenous injection, 72 hours, Inbred female Brown-Norway (BN) rats) results in the inhibition of antigen-induced infiltration of eosinophils and lymphocytes, but not neutrophils or monocytes, into the bronchoalveolar lavage fluid (BALF) of Brown-Norway (BN) rats. Animal model: Inbred female Brown-Norway (BN) rats and used at 4-6 weeks of age. Dosage: 0.01, 0.1, 1, 10 mg/kg. Administration: Intravenous injection; 72 hours. Result: Inhibited WBC and eosinophil infiltration in a dose-dependent manner.
• In Vitro:
  YM-90709 (0-100 μM; 1 hour) inhibits the binding of [125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells. YM-90709 (0-100 μM; 96 hour; Eosinophilic HL-60 clone 15 cells) affects IL-5 and GM-CSF and prolonged the survival time of eosinophils. YM-90709 (0-100 μM; 5 min; Eosinophilic HL-60 clone 15 cells) inhibits IL-5-induced, but not GM-CSF-induced, eosinophil survival as well as the tyrosine phosphorylation of Janus kinase 2.Cell Viability Assay Cell line: Purified eosinophils were suspended at 5x105 cells/ml in RPMI-1640 medium. Concentration: 0.01, 0.1, 1, 10 and 100 μM Incubation time: 96 hours. Result: The survival time of eosinophils was prolonged. Western blot analysis. Cell line: Eosinophilic HL-60 clone 15 cells in RPMI-1640 medium containing 10% FBS, antibiotics, 50 mM 2-ME and 25 mM HEPPES. Concentration: Incubation time: 5 min. Result: Reduced the IL-5-induced phosphorylation of JAK2 to near basal levels.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YM 90709 | YM90709

Quick Database Links

Gene Symbol

IL Receptor