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首页-小分子抑制剂&激动剂-GPCR-mAChR-VU 0365114
VU 0365114

Chemical Structure : VU 0365114

CAS No.: 1208222-39-2

VU 0365114 (VU-0365114, VU0365114)

货号: PC-21369Not For Human Use, Lab Use Only.

VU 0365114 is a selective type-5 muscarinic acetylcholine receptor (mAChR, M5) positive allosteric modulator (EC50=2.7 uM) and tubulin inhibitor by destabilizing microtubules, shows no activity against M1, M2, M3 and M4 receptors.

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

生物&药学活性

VU 0365114 is a selective type-5 muscarinic acetylcholine receptor (mAChR, M5) positive allosteric modulator (EC50=2.7 uM) and tubulin inhibitor by destabilizing microtubules, shows no activity against M1, M2, M3 and M4 receptors.
VU-0365114 exhibits a broad-spectrum in vitro anticancer activity, especially in colorectal cancer cells.
VU-0365114 slows the in vivo colorectal tumor growth in tumor xenograft study in nude mice.
VU 0365114 significantly increased electrically evoked DA release and the Oxo-M effect on DA release.

物理化学性质&存储条件

分子量 397.35
分子式 C22H14F3NO3
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

1-([1,1'-Biphenyl]-4-ylmethyl)-5-(trifluoromethoxy)indoline-2,3-dione

参考文献

1. Vivien Zell , et al. J Pharmacol Exp Ther. 2023 Nov;387(2):226-234.

2. Hsieh YY, et al. Mol Oncol. 2023 Oct 16. doi: 10.1002/1878-0261.13536.

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