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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Tryptophan 2,3-Dioxygenase (TDO)-NTRC 3531-0
NTRC 3531-0

Chemical Structure : NTRC 3531-0

CAS No.: 2171408-68-5

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NTRC 3531-0 (NTRC3531-0)

货号: 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.

规格 价格 库存 数量
2 mg ￥1580 In stock
5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 98.3% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 312.34
分子式 C18H17FN2O2
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

(S)-4-(6-fluoro-1H-indol-3-yl)-N-(1-hydroxypropan-2-yl)benzamide

参考文献

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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