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BRL-50481

CAS No. : 433695-36-4

MCE 国际站：BRL-50481

产品活性：BRL-50481 是 PDE7 的新型选择性抑制剂，对 PDE7A，PDE7B，PDE4 和 PDE3 的 IC₅₀ 值分别为 0.15，12.1，62 和 490 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

In Vitro: BRL-50481 increases the cAMP content (19.1±6.2% of IBMX response at 300 μM) but is considerably less potent. BRL-50481 (30 μM) fails to suppress proliferation by itself but significantly potentiates the effect of rolipram. BRL-50481 (30 μM) has no effect on IL-15-induced proliferation but augments the inhibitory effect of rolipram. Pretreatment (30 min) of human monocytes with BRL-50481 has, by itself, a negligible (~2 to 10%) inhibitory effect on TNFα output at all concentrations tested. BRL-50481 also potentiates the inhibitory effect of PGE₂ on LPS-induced TNFα release. BRL-50481 has no significant effect by itself on κB-dependent transcription (5.6±1.9% inhibition at 30 μM) and fails to enhance the effect of rolipram (maximum inhibition, 52.9±2.7%; pIC₃₀ value of 5.33±0.12). BRL-50481 suppresses, in a concentration-dependent manner, LPS-induced TNFα release in monocytes in which PDE7A1 is induced (21.7±1.6% inhibition at 30 μM at the 12-h time point).

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