
Bretazenil
CAS No. 84379-13-5
Bretazenil ( Ro 16-6028 )
产品货号. M27608 CAS No. 84379-13-5
Bretazenil 是一种 GABAA 苯二氮卓位点部分激动剂。 Bretazenil 对重组 α1β1γ2 的 EC50 为 10 nM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥591 | 有现货 |
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5MG | ¥907 | 有现货 |
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10MG | ¥1482 | 有现货 |
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25MG | ¥3224 | 有现货 |
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50MG | ¥4795 | 有现货 |
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100MG | ¥6845 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称Bretazenil
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注意事项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
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产品简述Bretazenil 是一种 GABAA 苯二氮卓位点部分激动剂。 Bretazenil 对重组 α1β1γ2 的 EC50 为 10 nM。
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产品描述Bretazenil is a GABAA benzodiazepine site partial agonist. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2.(In Vitro):Bretazenil was the most potent benzodiazepine examined, exhibiting an IC50 of 6.1 nM, compared to clonazepam (7.9 nM), flunitrazepam (13.6 nM) and diazepam (91.1 nM). The rank order of potency for inhibition of [35S]TBPS binding was identical to that for inhibition of [3H]flunitrazepam binding. However, Bretazenil was less efficacious in that it produced 27% inhibition of specific [35S]TBPS binding, compared to clonazepam (34%), flunitrazepam (41%) or diazepam (49%). Bretazenil antagonized the inhibition of [35S]TBPS binding produced by 10 microM diazepam. Bretazenil was also more potent and less efficacious than diazepam in potentiating GABA-stimulated 36Cl- uptake.(In Vivo):Bretazenil, was studied in 240 rats in five age groups: age 7, 12, 18, 25 and 90 days. Motor seizures induced by metrazol (pentamethylenetetrazol, PTZ, 100 mg/kg subcutaneously (s.c.) except for 18-day-old rats which received a dose of 90 mg/kg) served as a model. Animals were pretreated with Bretazenil in doses of 0.001-0.1 mg/kg intraperitoneally 10 min before metrazol. Both types of metrazol-induced seizures, minimal (mMS, predominantly clonic with preserved righting ability) and major (MMS, generalized tonic-clonic), were suppressed by Bretazenil in a dose-dependent manner. Major seizures were always more sensitive to Bretazenil than were minimal seizures. The youngest rats exhibited maximal effects of Bretazenil against major seizures. On the other hand, this drug increased the incidence of minimal seizures in 7- and 12-day-old rats, i.e., in age groups in which this type of seizure is rare under control conditions.
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体外实验——
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体内实验Bretazenil (0.001-0.1 mg/kg intraperitoneally 10 min before metrazol; age 7, 12, 18, 25 and 90 days male and female albino rats)suppresses both types of metrazol-induced seizures, minimal (mMS, predominantly clonic with preserved righting ability) and major (MMS, generalized tonic-clonic) in a dose-dependent manner.
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同义词Ro 16-6028
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通路Others
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靶点Other Targets
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受体——
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研究领域——
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适应症——
化学信息
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CAS Number84379-13-5
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分子量418.28
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分子式C19H20BrN3O3
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 50 mg/mL (119.54 mM)
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SMILESBrC1=C2C(N3[C@H](C4=C(C(OC(C)(C)C)=O)N=CN4C2=CC=C1)CCC3)=O
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Zhao F, et al. [Anthraquinones from the roots of Knoxia valerianoides]. Zhongguo Zhong Yao Za Zhi. 2011 Nov;36(21):2980-6. Chinese.
产品手册




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