YM-344484
YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca2+ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca2+ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis.
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- No. CAS: 671205-14-4
- Fòrmula: C28H30FN5O2
- Peso molecular:487.57
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Actividad biológica
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CCR3 |
H1 Receptor |
YM-344484 potently inhibits CCR3 ligand-induced calcium influx in B300-19 cells expressing human CCR3, with its Kβ values ranging from 0.69 nM to 2.5 nM depending on the ligand[1].
YM-344484 inhibits CCL11-induced calcium influx in mouse CCR3-expressing cells, with a Kβ value of 88 nM[1].
YM-344484 inhibits histamine H1 receptor-mediated calcium influx in PC3 cells, with a Kβ value of 47 nM[1].
YM-344484 (10 μM) exhibits only weak inhibitory activity against serotonin 5-HT2A receptor-mediated calcium influx in C6 cells, with an inhibition rate of merely 25%[1].
YM-344484 potently inhibits CCR3 ligand-induced chemotaxis in human CCR3-expressing B300-19 cells, with its IC50 values ranging from 2.0 nM to 8.0 nM depending on the ligand[1].
YM-344484 inhibits the release of eosinophil-derived neurotoxin from human peripheral blood eosinophils induced by CCL11, with an IC50 value of 19 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
YM-344484 (100-600 mg/kg; p.o.; once every 8 hours; 6 doses total) inhibits eosinophil infiltration by 74% at the dose of 300 mg/kg, and completely suppresses eosinophil infiltration at the dose of 600 mg/kg, in a mouse asthma model induced by Ovalbumins (HY-W250978)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 6 weeks old)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Suppressed histamine-induced vascular permeability dose-dependently.
Achieved statistically significant 82% inhibition at 10 mg/kg.
Achieved complete inhibition at 30 mg/kg.
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Animal Model:Balb/c (female)[1]
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Dosage:100 mg/kg; 300 mg/kg; 600 mg/kg
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Administration:p.o.; every 8 hours; 6 doses
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Result:Failed to reduce eosinophil numbers at 100 mg/kg.
Significantly attenuated eosinophil infiltration with 74% inhibition at 300 mg/kg.
Achieved 100% inhibition of eosinophil infiltration at 600 mg/kg.
Exhibited no inhibitory effect on neutrophil or mononuclear cell counts in bronchoalveolar lavage fluid.
Chemical Information
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No. CAS 671205-14-4
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Peso molecular 487.57
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Fòrmula C28H30FN5O2
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SMILES
FC(C=C1)=CC(C=C2)=C1C=C2CN3C[C@@H](CC3)NC(/C=C4CCN(CC/4)C(C5=CC=C(N=N5)C)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YM-344484 Related Classifications
HY-182736 Related Classifications
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