BRL-50481

产品编号 T5106Cas号 433695-36-4

别名

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。

为众多的药物研发团队赋能，

让新药发现更简单！

产品编号 T5106Cas号 433695-36-4

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。

大包装 & 定制

加入购物车

实验操作小课堂

选择批次:

纯度:99.89%

联系我们获取更多批次信息

资源下载

TargetMol 的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

生物活性

产品描述	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.
靶点活性	PDE3:490 μM, PDE7A:0.15 μM, PDE7B:12 μM, PDE4:62 μM
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].
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].

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

Ethanol: 20 mg/mL

DMSO: 45 mg/mL (184.22 mM)

溶液配制表

DMSO