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Submit ReviewNF 1819 is a potent and selective irreversible MAGL inhibitor (IC50 values are 0.25 and 7.4 nM at rMAGL and hMAGL, respectively). Exhibits 389-fold selectivity over hFAAH and exhibits minimal binding at CB receptors (IC50 > 10 μM). Alleviates symptoms in a MS in vivo model. Exhibits analgesic effects in an acute inflammatory pain model in vivo. Ameliorates neuropathic hypersensitivity induced by oxaliplatin (Cat. No. 2623). Displays high membrane permeability and brain penetrant.
分子量 | 463.46 |
公式 | C24H22FN5O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1881244-28-5 |
PubChem ID | 127032456 |
InChI Key | XRIROGBLGLPXQI-FGZHOGPDSA-N |
Smiles | FC1=CC=C([C@@H]2[C@@H](C3=CC=C4OCOC4=C3)N(C2=O)C5CCN(C(N6C=NC=N6)=O)CC5)C=C1 |
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Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Brindisi et al (20106) Development and pharmacological characterization of selective blockers of 2-arachidonoyl glycerol degradation with efficacy in rodent models of multiple sclerosis and pain. J.Med.Chem. 59 2612 PMID: 26888301
关键词: NF 1819, NF 1819 supplier, NF1819, Potent, selective, irreversible, MAGL, inhibitors, inhibits, MS, multiple, sclerosis, analgesics, neuropathic, hypersensitivity, membrane, permeable, brain, penetrant, 5956, Tocris Bioscience
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