BRL 50481

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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

BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15 12.1 62 and 490 μM for PDE7A PDE7B PDE4 and PDE3 respectively.

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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Angiogenesis

PDE

PDE7

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433695-36-4

244.27

C9H12N2O4S

>98% (HPLC)

DMSO: 100 mg/mL;Ethanol: 20 mg/mL

CN(C)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O

NN2-Trimethyl-5-nitro-benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years