CPPHA

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

CPPHA 是一种高效、选择性的代谢型谷氨酸受体 mGluR5 和 mGluR1 正向变构调制器 (PAM)。CPPHA 可增强 mGluR5 和 mGluR1 对受体激活的反应。CPPHA 被开发用于中枢神经系统疾病的研究。

CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.

CPPHA alone has no agonist activity.CPPHA causes concentration-dependent potentiation of the response of human mGluR5 CHO cells to agonists.CPPHA potentiates threshold response to glutamate in fluorometric Ca2+ assays 7- to 8-fold with EC50 values in the 400 to 800 nM range.CPPHA (20 μM; 15 minutes) potentiates the response to a subthreshold concentration of DHPG (HY-12598A) on ERK and cyclic-AMP responsive element-binding protein (CREB) activity, as well as NMDA receptor subunit NR1 phosphorylation in cortical and hippocampal slices.Cell Line:Rat hippocampal cells Concentration:20 μM Incubation Time:15 minutes Result: Potentiated the DHPG (20 μM)-induced increase in phosphorylation of ERK and CREB, approaching levels seen with 100 μM DHPG alone.

——

——

Neuroscience

GluR

GluR

——

——

693288-97-0

406.82

C22H15ClN2O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (245.81 mM; 超声助溶 )

Oc1ccccc1C(=O)Nc1ccc(Cl)cc1CN1C(=O)c2ccccc2C1=O

——

(-20℃)

With Ice Pack

≥ 2 years