CPPHA

Research use only, not for human use.

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

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.

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Neuroscience

GluR

GluR

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693288-97-0

406.82

C22H15ClN2O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (245.81 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years