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首页-小分子抑制剂&激动剂-GPCR-mGluR-DFMTI
DFMTI

Chemical Structure : DFMTI

CAS No.: 864864-86-8

DFMTI (MK-5435, MK5435)

货号: PC-42136Not For Human Use, Lab Use Only.

DFMTI (MK5435) is a potent, selective, brain penetrant and orally active mGluR1 antagonist with 4.3 nM and 3.6 nM for huam and rat mGluR1, respectively.

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

生物&药学活性

DFMTI (MK5435) is a potent, selective, brain penetrant and orally active mGluR1 antagonist with 4.3 nM and 3.6 nM for huam and rat mGluR1, respectively.
DFMTI displasy liitle to no activity for mGluR5, mGluR2 and mGluR8.
DFMTI has improved in vivo DMPK profiles and shows antipsychotic-like effect at a dose of 1 mg/kg in an animal model.

物理化学性质&存储条件

分子量 368.3799
分子式 C20H18F2N4O
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

1H-Isoindol-1-one, 5-[1-(2,4-difluorophenyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-2-(1-methylethyl)-

参考文献

1. Ito S, et al. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5310-3.

2. Cho HP, et al. ACS Chem Neurosci. 2014 Jul 16;5(7):597-610.

3. Satoh A, et al. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5464-8.

4. Hostetler E, et al. Synapse. 2011 Feb;65(2):125-35.

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