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Chemical Structure : NTRC 3531-0
CAS No.: 2171408-68-5
Catalog No.: PC-49664Not For Human Use, Lab Use Only.
NTRC 3531-0 is a brain-penetrable, selective inhibitor of L-tryptophan-catabolizing enzyme tryptophan 2,3-dioxygenase (TDO) with IC50 of 490 nM (hTDO) in biochemical assays and cellular IC50 of 816 nM in HEK-hTDO.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $158 | In stock | |
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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NTRC 3531-0 is a brain-penetrable, selective inhibitor of L-tryptophan-catabolizing enzyme tryptophan 2,3-dioxygenase (TDO) with IC50 of 490 nM (hTDO) in biochemical assays and cellular IC50 of 816 nM in HEK-hTDO.
NTRC 3531-0 is inactive on hIDO1 in the biochemical assay at >30 uM, inhibits Trp metabolism in human IDO1-overexpressing HEK-293 cells (HEK-hIDO1) with an IC50 of 20.7 µM, 60 times selective for hTDO over hIDO1.
NTRC 3531-0 is slightly less potent on mTDO compared to hTDO in the biochemical assays (mTDO IC50=846 nM).
Oral administration of NTRC 3531-0 (100 mg/kg) resulted in an increase in the concentration of Trp in plasma as well as in brain compared to mice treated with vehicle.
NTRC 3531-0 treatment showed decreased expression of rotenone‐induced glial fibrillary acidic protein (GFAP), which is a marker of enteric glial cells, and decreased α‐synuclein accumulation in the enteric plexus.
| M.Wt | 312.34 | |
| Formula | C18H17FN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-4-(6-fluoro-1H-indol-3-yl)-N-(1-hydroxypropan-2-yl)benzamide |
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1. Perez-Pardo P, et al. FEBS J. 2021 Jul;288(14):4311-4331.
2. Patent Application No. WO2018/011227 A1.
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