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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).

Images & Validation

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YM-90709

Key Properties

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CAS Number163769-88-8
MW359.4211
Purity>98% (HPLC)
FormulaC22H21N3O2
SMILESCC(CC1=CC(OC)=C(OC)C=C12)(C)N3C2=CC4=NC5=CC=CC=C5N=C43
TargetIL Receptor
Solubility10 mM in DMSO

Bioactivity

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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

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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YM 90709 | YM90709

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  • YM-90709

    YM-90709 [orb1304505]

    >99.99% (May vary between batches)

    163769-88-8

    359.42

    C22H21N3O2

    50 mg, 1 mg, 5 mg, 10 mg, 25 mg, 100 mg, 1 ml x 10 mM (in DMSO)
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Gene Symbol
IL Receptor

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