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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-P2X Receptor-(Rac)-EVT-401
(Rac)-EVT-401

Chemical Structure : (Rac)-EVT-401

CAS No.:

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(Rac)-EVT-401 (EVT401, EVT-401)

货号: PC-26954Not For Human Use, Lab Use Only.

(Rac)-EVT-401 is the racemate form of EVT-401, a potent, highly selective human P2X7 receptor (P2X7R) antagonist with Ki of 7.6 nM in competitive binding assays.

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

    生物&药学活性

    (Rac)-EVT-401 is the racemate form of EVT-401, a potent, highly selective human P2X7 receptor (P2X7R) antagonist with Ki of 7.6 nM in competitive binding assays.
    EVT-401 differentially inhibits P2X7R-mediated calcium influx in 1321N1 cells expressing human and rat P2X7R with IC50 of 10 nM for hP2X7R and 220 nM for rat P2X7R.
    EVT-401 does not inhibit the functions of P2X7-related P2 receptors (P2X1R, P2X2R, P2X3R, and P2X4R).
    EVT-401 (100 uM) inhibits the proliferation of rheumatoid arthritis synovial fibroblasts (RA SF) by inducing G1 cell cycle arrest.
    EVT-401 interferes with the inflammatory phenotypes of RA SF. EVT-401 significantly reduced the clinical arthritis score, diminished swelling in proximal interphalangeal (PIP) joints, and decreased the incidence of PIP arthriti in NHP arthritis.

    物理化学性质&存储条件

    分子量 436.41
    分子式 C22H20F4N2O3
    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

    2-(3-fluoro-4-(trifluoromethyl)phenyl)-N-(2-(1-hydroxypropan-2-yl)-6-methyl-1-oxo-1,2-dihydroisoquinolin-5-yl)acetamide

    参考文献

    1. Rao P, et al. Sci Adv. 2026 May 22;12(21):eadw9543.

    2. Zhu B, et al. J Pharm Anal. 2017 Aug;7(4):223-230.

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