233275-76-8|MK 0343|CsnPharm

CAS No.: 233275-76-8

MK-0343 Catalog No. CSN19855

Synonyms: MRK-409

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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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 GABAA Receptor α3

Ki:0.21 Adrenergic Receptor α1

Ki:0.22 GABAA Receptor α5

Ki:0.23 GABAA Receptor α2

Ki:0.4
描述GABA (γ-aminobutyric acid) receptors, of which there are two types, are involved in inhibitory synapses within the central nervous system. The GABA_A 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 GABA_A 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 GABA_A 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].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03094637	Hematopoietic/Lymphoid Cancer ... more >> Myelodysplastic Syndrome Collapse <<	Phase 2	Recruiting	November 2022	United States, Texas ... more >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact ggarciam@mdanderson.org Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5165 mL
- 12.5824 mL
- 25.1647 mL
- 5 mM
- 0.5033 mL
- 2.5165 mL
- 5.0329 mL
- 10 mM
- 0.2516 mL
- 1.2582 mL
- 2.5165 mL

技术信息

CAS号	233275-76-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C19H17F2N7O	运输	蓝冰
分子量	397.38	别名	MRK-409

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靶点	Description	IC50
GABAA Receptor α3		Ki:0.21
Adrenergic Receptor α1		Ki:0.22
GABAA Receptor α5		Ki:0.23
GABAA Receptor α2		Ki:0.4

MK-0343 Catalog No. CSN19855

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