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首页-小分子抑制剂&激动剂-Others-Other Targets-Padsevonil
Padsevonil

Chemical Structure : Padsevonil

CAS No.: 1294000-61-5

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Padsevonil (UCB-0942, UCB0942)

货号: PC-35479Not For Human Use, Lab Use Only.

Padsevonil (UCB0942) is an antiepileptic drug (AED) candidate with high affinity for synaptic vesicle 2 (SV2) proteins with pKi of 8.5/7.9/8.5 for SV2A/SV2B/SV2C, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Padsevonil (UCB0942) is an antiepileptic drug (AED) candidate with high affinity for synaptic vesicle 2 (SV2) proteins with pKi of 8.5/7.9/8.5 for SV2A/SV2B/SV2C, respectively.
Padsevonil (UCB0942) displayed low to moderate affinity (pIC50≤6.1) for the benzodiazepine site of recombinant GABAA receptors.
Padsevonil (UCB0942) exhibited SV2A occupancy at low ED50 (0.2 mg/kg) and benzodiazepine site occupancy at higher doses (ED50 36 mg/kg) in in vivo (mice) receptor occupancy studies.
Padsevonil (UCB0942) is a first-in-class AED candidate with a unique target profile allowing for presynaptic and postsynaptic activity.

物理化学性质&存储条件

分子量 432.794
分子式 C14H14ClF5N4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-4-(2-chloro-2,2-difluoroethyl)-1-((2-(methoxymethyl)-6-(trifluoromethyl)imidazo[2,1-b][1,3,4]thiadiazol-5-yl)methyl)pyrrolidin-2-one

参考文献

1. Serrano E, et al. F1000Prime Rep. 2015 May 26;7:61.

2. Zaccara G, et al. Pharmacol Res. 2016 Feb;104:38-48.

3. Wood M, et al. J Pharmacol Exp Ther. 2020. PMID: 31619465

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