Fenobam 是一种选择性、口服活性、能穿透血脑屏障的 mGluR5 拮抗剂,作用于别构调节位点(在大鼠和人重组 mGlu5 受体上的 Kd 值分别为 54 nM 和 31 nM)。Fenobam 具有反向激动剂活性,IC50 为 84 nM,阻断 mGlu5 受体活性,具有抗焦虑作用。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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描述 | Fenobam is a selective, orally active antagonist of mGluR5 with an IC50 of 84 nM and the ability to cross the blood-brain barrier. The Kd values of Fenobam for rat and human recombinant mGlu5 receptors are 54 nM and 31 nM, respectively. Fenobam exhibits anti-anxiety properties, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. It is used in research related to neurological disorders, cancer, and drug addiction[1][2][3]. At a concentration of 300 μM, a 72-hour treatment with Fenobam significantly inhibits the proliferation of LM7 cells and induces apoptosis[2]. |
Animal study | Administered orally at doses of 30-60 mg/kg three times a week, Fenobam significantly suppresses self-administration behavior in rats[3]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01981395 | Hyperalgesia ... 展开 >>Allodynia 收起 << | Phase 1 | Completed | - | United States, Missouri ... 展开 >> Washington University School of Medicine St. Louis, Missouri, United States, 63110 收起 << |
NCT01806415 | Healthy | Phase 1 | Completed | - | United States, Missouri ... 展开 >> Washington University School Of Medicine St. Louis, Missouri, United States, 63110 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.75mL 0.75mL 0.37mL |
18.75mL 3.75mL 1.87mL |
37.50mL 7.50mL 3.75mL |
CAS号 | 57653-26-6 |
分子式 | C11H11ClN4O2 |
分子量 | 266.684 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(393.72 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |