LDDN-0003499
LDDN-0003499 is a Src family tyrosine kinase inhibitor and anti-inflammatory agent. LDDN-0003499 reduces basal and Aβ-stimulated levels of active, phosphorylated Lyn and Src kinases, and attenuates Aβ-stimulated secretion of pro-inflammatory cytokines TNFα and IL-6 in microglial cells. LDDN-0003499 can be used for the research of Alzheimer's disease.
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- CAS No.: 331662-51-2
- Formule: C16H13Cl2N3O2
- Masse moléculaire:350.20
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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IL-6 |
LDDN-0003499 (0.5 nM-50 μM; 24 h) shows no toxicity to mouse microglial BV2 cells[1].
LDDN-0003499 (0.5 nM-50 μM; 1 h) reduces the total protein phosphotyrosine level in murine microglial BV2 cells in a dose-dependent manner[1].
LDDN-0003499 (0.5 nM-50 μM; 1 h) dose-dependently inhibits the basal activity levels of phosphorylated Lyn and Src in mouse microglial BV2 cells[1].
LDDN-0003499 (0.5 nM-50 μM; 65 min) dose-dependently inhibits the Aβ-induced increase in the levels of activated phosphorylated Lyn and Src in mouse microglial BV2 cells[1].
LDDN-0003499 (0.5 nM-50 μM; 1 h) reduces Aβ-stimulated secretion of TNF-α and IL-6 in mouse microglial BV2 cells in a dose-dependent manner[1].
LDDN-0003499 (1 μM) exhibits moderately high NADPH-dependent clearance and low non-NADPH-dependent clearance in human and mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:unstimulated murine microglial BV2 cells
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Concentration:0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM, 50 μM
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Incubation Time:1 h
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Result:Produced a dose-dependent decrease in active, phosphorylated Lyn (pLyn) and Src (pSrc) protein levels.
Did not alter phosphorylated levels of ERK, JNK, or p38.
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Cell Line:Aβ-stimulated murine microglial BV2 cells
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Concentration:0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM, 50 μM
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Incubation Time:1 h (pre-incubation); 5 min (co-incubation with 1 μM Aβ1-42)
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Result:Attenuated the Aβ-stimulated increase in active, phosphorylated Lyn and Src protein levels.
Significantly attenuated the Aβ-stimulated increase in pLyn at 50 nM, while 500 nM was required for pSrc, demonstrating 10-fold selectivity for Lyn over Src in this paradigm.
Did not inhibit Aβ-stimulated increases in phosphorylated ERK.
Chemical Information
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CAS No. 331662-51-2
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Masse moléculaire 350.20
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Formule C16H13Cl2N3O2
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SMILES
ClC1=CC=C(NC=2N=CN=C3C=C(OC)C(OC)=CC32)C(Cl)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LDDN-0003499 Related Classifications
HY-112369 Related Classifications
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