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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Monoamine Transporter-JNT-517
JNT-517

Chemical Structure : JNT-517

CAS No.: 2837993-05-0

JNT-517 (Repinatrabit, JNT517)

货号: PC-25026Not For Human Use, Lab Use Only.

JNT-517 (Repinatrabit, JNT517) is a highly selective, first-in-class, orally bioavailable inhibitor of SLC6A19 (B0AT1) with IC50 of 47 nM against human SLC6A19 in the isoleucine transport assay.

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

生物&药学活性

JNT-517 (Repinatrabit, JNT517) is a highly selective, first-in-class, orally bioavailable inhibitor of SLC6A19 (B0AT1) with IC50 of 47 nM against human SLC6A19 in the isoleucine transport assay.
JNT-517 (Repinatrabit) potently inhibitsthe transport of glutamine in human intestinal epithelial cells with endogenous expression levels of SLC6A19 (IC50 = 81 nM).
JNT-517 (Repinatrabit) does not inhibit either SLC1A5, SLC7A5, or SLC6A8 at 35 uM.
JNT-517 (Repinatrabit) also shows negligible activity against mouse SLC6A19 (IC50>11.8 uM).
JNT-517 (Repinatrabit) is found to be safe and well tolerated and increased the urinary excretion of Phe in a phase 1 healthy volunteer study.

物理化学性质&存储条件

分子量 418.39
分子式 C18H22F4N4O3
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

(R)-3-(1-Cyclopropyl-3-(2-fluoro-4-(trifluoromethoxy)benzyl)ureido)piperidine-1-carboxamide

参考文献

1. Wobst HJ, et al. JCI Insight. 2024 Nov 8;9(21):e182876.

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