Identification | Back Directory | [Name]
5,6-DIHYDRO-2,3-DIMETHOXY-6,6-DIMETHYLBENZ[7,8]INDOLIZINO[2,3-B]QUINOXALINE | [CAS]
163769-88-8 | [Synonyms]
YM 90709 YM 90709;YM90709;YM-90709 5,6-DIHYDRO-2,3-DIMETHOXY-6,6-DIMETHYLBENZ[7,8]INDOLIZINO[2,3-B]QUINOXALINE 2,3-Dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline Benz[7,8]indolizino[2,3-b]quinoxaline,5,6-dihydro-2,3-dimethoxy-6,6-dimethyl- | [Molecular Formula]
C22H21N3O2 | [MDL Number]
MFCD00354370 | [MOL File]
163769-88-8.mol | [Molecular Weight]
359.42 |
Chemical Properties | Back Directory | [Boiling point ]
579.6±50.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Room Temperature | [solubility ]
DMF: 10 mg/ml; DMSO: 20 mg/ml; Ethanol: 2 mg/ml | [form ]
A crystalline solid | [pka]
2.74±0.40(Predicted) | [color ]
Brown to orange |
Hazard Information | Back Directory | [Description]
YM-90709 is a competitive antagonist of the interleukin-5 (IL-5) receptor that has IC50 values of 1 and 0.57 μM for peripheral human eosinophils and eosinophilic HL-60 clone 15 cells, respectively, in a radioligand binding assay. It inhibits IL-5-induced eosinophil survival (IC50 = 0.45 μM) and JAK2 phosphorylation in vitro. YM-90709 inhibits eosinophil and lymphocyte infiltration (ED50s = 0.32 and 0.12 mg/kg, respectively) into the brochoalveolar lavage fluid (BALF) of rats and eosinophil infiltration (ED50 = 0.05 mg/kg) into the BALF of mice in models of airway inflammation. | [Uses]
YM 90709, is an interleukin-5 receptor antagonist. | [Definition]
ChEBI: LSM-2128 is a quinoxaline derivative. | [Biological Activity]
Novel, selective inhibitor of interleukin-5 (IL-5) binding to its receptor (IC 50 = 0.45-1 mM). Inhibits IL-5-prolonged eosinophil survival and IL-5-induced tyrosine phosphorylation of JAK2 without inhibiting GM-CSF-mediated effects. In vivo, inhibits antigen-induced eosinophil and lymphocyte recruitment in rat airways, without affecting peripheral blood or bone marrow leukocytes. | [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[2]. Animal Model: | Inbred female Brown-Norway (BN) rats and used at 4-6 weeks of age[2]. | 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. |
| [IC 50]
IL-5 |
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