價格 | ¥203 | ¥359 | ¥797 |
包裝 | 5mg | 10mg | 25mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2025-07-28 |
中文名稱:化合物 CPPHA | 英文名稱:CPPHA |
CAS:693288-97-0 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
純度規(guī)格: 99.61% | 產(chǎn)品類別: 抑制劑 |
貨號: T10881 |
名稱 | CPPHA |
描述 | CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases. |
細(xì)胞實驗 | CPPHA potentiated the response to a subthreshold concentration of 3,5-dihydroxy-phenylglycine (DHPG) on extracellular signal-regulated protein kinase (ERK) and cyclic-AMP responsive element-binding protein (CREB) activity, as well as N-methyl d-aspartate (NMDA) receptor subunit NR1 phosphorylation in cortical and hippocampal slices [1]. CPPHA potentiated threshold responses to glutamate in fluorometric Ca(2+) assays 7- to 8-fold (EC50s: 400 to 800 nM), and at 10 μM shifted mGluR5 agonist concentration-response curves to glutamate, quisqualate, and DHPG 4- to 7-fold to the left. CPPHA (10 μM) potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself. Similarly, 10 μM CPPHA also potentiated mGluR5-mediated DHPG-induced depolarization of rat subthalamic nucleus neurons [2]. CPPHA induced an increase in basal mGluR5-mediated ERK1/2 phosphorylation and potentiated the effect of low concentrations of agonists. In contrast, CPPHA significantly decreased ERK1/2 phosphorylation induced by high concentrations of agonists [3]. |
體外活性 | CPPHA增強(qiáng)了亞閾濃度的3,5-二羥基苯甘氨酸(DHPG)對細(xì)胞外信號調(diào)節(jié)蛋白激酶(ERK)和cAMP響應(yīng)元件結(jié)合蛋白(CREB)活性的影響,以及在皮層和海馬切片中的N-甲基-D-天門冬氨酸(NMDA)受體亞單位NR1的磷酸化[1]。CPPHA將熒光Ca(2+)測定中對谷氨酸的閾反應(yīng)增強(qiáng)了7至8倍(EC50s:400至800nM),并在10微摩爾濃度下將mGluR5激動劑對谷氨酸、鹿蕨酸和DHPG的濃度反應(yīng)曲線向左移動了4至7倍。10微摩爾的CPPHA增強(qiáng)了海馬切片中由DHPG誘導(dǎo)的NMDA受體電流,盡管它本身對這些電流沒有影響。同樣,10微摩爾的CPPHA也增強(qiáng)了大鼠下丘腦神經(jīng)元DHPG誘發(fā)的mGluR5介導(dǎo)的去極化[2]。CPPHA提升了基礎(chǔ)mGluR5介導(dǎo)的ERK1/2磷酸化水平,并增強(qiáng)了低濃度激動劑的效應(yīng)。相比之下,CPPHA顯著降低了高濃度激動劑誘導(dǎo)的ERK1/2磷酸化[3]。 |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
溶解度 | DMSO : 90.0 mg/mL (221.2 mM), Sonication is recommended. |
關(guān)鍵字 | mGluR5 | mGluR1 | CPPHA |
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相關(guān)庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 神經(jīng)信號分子庫 | 谷氨酰胺代謝化合物庫 | 神經(jīng)退行性疾病化合物庫 | 膜蛋白靶向化合物庫 |
成立日期 | 2013-04-18 (13年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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