VU 6001966 |
カタログ番号GC50612 |
VU 6001966 (化合物 15m) は、血液脳関門 mGlu2 (代謝型グルタミン酸受容体 2) を通過する強力なアロステリック モジュレーターであり、mGlu2 と mGlu3 の IC50 はそれぞれ 78 nM と >30 μM です。
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Cas No.: 2009052-76-8
Sample solution is provided at 25 µL, 10mM.
Potent and selective mGlu2 negative allosteric modulator (IC50 = 78 nM). Exhibits > 350-fold selectivity for mGlu2 over mGlu3. Also exhibits selectivity over other mGluRs and a panel of GPCRs, ion channels and transporters. CNS penetrant.
Bollinger et al (2017) Design and synthesis of mGlu2 NAMs with improved potency and CNS penetration based on a truncated picolinamide core. ACS Med.Chem.Lett. 8 919 PMID:28947937
Average Rating: 5
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