化合物BRL 50481 T5106

Product Introduction
Bioactivity


英文名: BRL-50481

描述: BRL 50481 是一种新型的、选择性的 PDE7 的抑制剂，对 PDE7A，PDE7B，PDE4和 PDE3的 IC50值分别为 0.15，12.1，62 和 490 μM。

细胞实验: MOLT-4 cells in 96-well plates are treated for 30 min with BRL-50481. The cAMP content is then determined by an immuno-specific ELISA. Results are expressed as a percentage of the response affected by 100 μM IBMX[2].

体外活性: 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) [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 20 mg/mL
DMSO : 45 mg/mL (184.22 mM)


关键字: BRL-50481 | inhibit | BRL50481 | Inhibitor | BRL 50481 | Phosphodiesterase (PDE)

相关产品: Torbafylline | Zatolmilast | PDE IV-IN-1 | BAY 2666605 | MR-L2 | Dasantafil | CALP2 acetate(261969-04-4 free base) | Ro 20-1724 | Theophylline monohydrate | Rolipram

相关库: Anti-Neurodegenerative Disease Compound Library | Bioactive Lipid Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | Metabolism Compound Library | Anti-Alzheimer's Disease Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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