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。
| 生物活性 | CPPHA is potent and selective positive allosteric modulator (PAM) of themGluR5andmGluR1(metabotropic glutamate receptor). CPPHA can potentiate responses ofmGluR5andmGluR1to activation of these receptors. CPPHA is developed for the research of central nervous system disorders[1][2]. |
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体外研究
(In Vitro) | CPPHA alone has no agonist activity[1].
CPPHA causes concentration-dependent potentiation of the response of human mGluR5 CHO cells to agonists[1].
CPPHA potentiates threshold response to glutamate in fluorometric Ca2+assays 7- to 8-fold with EC50values in the 400 to 800 nM range[1].
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[3].
Western Blot Analysis[3] | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(245.81 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4581 mL | 12.2904 mL | 24.5809 mL | | 5 mM | 0.4916 mL | 2.4581 mL | 4.9162 mL | | 10 mM | 0.2458 mL | 1.2290 mL | 2.4581 mL |
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