货号:A212464 同义名: MRK-409 产品仅供科研
MK 0343 is a selective partial agonist of GABAAα3, α1, α5 and α2 with Ki values of 0.21 nM-0.40 nM. It displays anxiolytic activity in rodent and primate models.
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产品名称 | GABA receptor ↓ ↑ | GABAA receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Niflumic Acid | ✔ | 98% | |||||||||||||||||
Ginkgolide A |
++
GABA receptor, Ki: 14.5 μM |
98% | |||||||||||||||||
Valproic acid sodium | ✔ | Autophagy,HDAC | 97% | ||||||||||||||||
Flumazenil | ✔ | 95% | |||||||||||||||||
Bemegride | ✔ | 98% | |||||||||||||||||
Bicuculline |
+++
GABAA receptor, IC50: 2 μM |
98+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | GABA (γ-aminobutyric acid) receptors, of which there are two types, are involved in inhibitory synapses within the central nervous system. The GABAA receptor (GABAAR) has a central role in modern anesthesia and sedation practice, which is evident from the high proportion of agents that target the GABAAR[3]. MK-0343 binds to α1-, α2-, α3- and α5-containing human recombinant GABAA receptors with comparable high affinity (0.21-0.40 nM)[4]. This compound readily penetrates the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL[4]. MK-0343 causes sedation in humans at a dose of 2 mg, corresponding to levels of occupancy considerably less than those predicted from rodent models to be required for anxiolytic efficacy (∼35-65%)[4]. MK-0343 0.75 mg was equipotent with lorazepam as indicated by saccadic peak velocity (SPV) (-42.4 deg/s), saccadic latency (0.02 s) and Visual Analogue scales (VAS) alertness scores (1.50 ln mm), while effects on memory and postural stability were smaller[5]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.58mL 2.52mL 1.26mL |
25.16mL 5.03mL 2.52mL |
CAS号 | 233275-76-8 |
分子式 | C19H17F2N7O |
分子量 | 397.381 |
别名 | MRK-409 |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 250 mg/mL(629.12 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 |