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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-VU0810464
VU0810464

Chemical Structure : VU0810464

CAS No.: 2126040-21-7

VU0810464 (VU 0810464;VU464)

货号: PC-36154Not For Human Use, Lab Use Only.

VU0810464 (VU 0810464, VU464) is a selective neuronal GIRK channels activator, displays nanomolar potency for GIRK1/2 (EC50=163 nM) and improved brain penetration.

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

生物&药学活性

VU0810464 (VU 0810464, VU464) is a selective neuronal GIRK channels activator, displays nanomolar potency for GIRK1/2 (EC50=163 nM) and improved brain penetration.
VU0810464 exhibits comparable efficacy and potency compared with ML297, but VU0810464 is more selective for neuronal GIRK channels (GIRK1/4 EC50>500 nM).
VU0810464 displays >3-fold more potent on GIRK1/2-expressing HEK293 cells compared to GIRK1/4-expressing cells, as measured using a Tl+ flux assay.
VU0810464 reduced stress-induced hyperthermia in a GIRK-dependent manner in mice, ML297, but not VU0810464, decreased anxiety-related behavior as assessed with the elevated plus maze test.

物理化学性质&存储条件

分子量 349.834
分子式 C18H21ClFN3O
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

2-(3-chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide

参考文献

1. Vo BN, et al. Br J Pharmacol. 2019 Mar 29. doi: 10.1111/bph.14671.

2. Wieting JM, et al. ACS Chem Neurosci. 2017 Sep 20;8(9):1873-1879.

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