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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-LY3526318
LY3526318

Chemical Structure : LY3526318

CAS No.: 1889218-34-1

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LY3526318 (LY-3526318)

货号: PC-23622Not For Human Use, Lab Use Only.

LY3526318 is a potent, selective, and orally bioavailable TRPA1 antagonist, inhibits human TRPA1 channel-mediated inward currents with IC50 of 13.5 nM.

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

生物&药学活性

LY3526318 is a potent, selective, and orally bioavailable TRPA1 antagonist, inhibits human TRPA1 channel-mediated inward currents with IC50 of 13.5 nM.
LY3526318 also potently inhibits rat, dog, and cynomolgus monkey TRPA1 with IC50 of 55.7, 7.6 and 8.2 nM respectively.
LY3526318 is highly selective for the blockade of TRPA1 ion channel function, with IC50s > 32 µM across a panel of other ion channels.
LY3526318 inhibits CA-induced calcium responses in IMR-32 cells with IC50 of 0.82 nM, >10-fold more potent than comparator TRPA1 antagonists, A-967079, ruthenium red, and HC-030031.
LY3526318 potently inhibits CA-evoked release of CGRP from rat DRG cultured neurons with IC50 of 27.1 nM using an ELISA assay.
LY3526318 blocks formalin-evoked flinching behaviors and chronic Freund adjuvant–induced cold hypersensitivity in rats.

物理化学性质&存储条件

分子量 556.47
分子式 C23H19F3N10O4
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)-2-(3-methyl-1-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-(2-(trifluoromethyl)pyrimidin-5-yl)pyridin-2-yl)propanamide

参考文献

1. Bamps D, et al. Clin Pharmacol Ther. 2023 Nov;114(5):1093-1103.
2, Broad LM, et al. Pain. 2025 Apr 18. doi: 10.1097/j.pain.0000000000003570.

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