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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-ELP-004
ELP-004

Chemical Structure : ELP-004

CAS No.: 15533-81-0

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ELP-004 (ELP004)

货号: PC-23865Not For Human Use, Lab Use Only.

ELP-004 is a small molecule inhibitor of transient receptor potential canonical (TRPC) channels, inhibits TRPC channel–mediated Ca2+ entry with high potency, preferentially inhibits inflammatory cytokine-induced pathological osteoclastogenesis.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ELP-004 is a small molecule inhibitor of transient receptor potential canonical (TRPC) channels, inhibits TRPC channel–mediated Ca2+ entry with high potency, preferentially inhibits inflammatory cytokine-induced pathological osteoclastogenesis.
ELP-004 potently inhibits OAG stimulated rapid Ca2+ entry in untreated TRPC3/6/7-expressing cells with IC50 of 1-2 uM, suppresses the increase in Fura2 ratios caused by subsequent additions of Sr2+ (3 mM) in both TRPC4- and TRPC5-expressing cells by 1 to 2 orders of magnitude (IC50 = 11.5 nM for TRPC5 and 172.4 nM for TRPC4).
ELP-004 is an allosteric modulator with both inhibitory and facilitatory (at higher concentrations) effects on the TRPC4 channel.
ELP-004 inhibits basal Ca2+ and related NFATc1 translocation in inflammatory cytokine-dependent osteoclastogenesis, has minimal effect on RANKL-induced osteoclastogenesis.
ELP-004 blocks TNFα-induced osteoclast fusion.ELP-004 inhibits osteoclastogenesis in human cells, ELP-004 also reduces bone erosion in a mouse model of rheumatoid arthritis.

物理化学性质&存储条件

分子量 232.10
分子式 C10H11Cl2NO
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

N-(3,4-dichlorophenyl)-N-methylpropionamide

参考文献

1. Ray S, et al. Sci Adv. 2025 Jan 17;11(3):eabm9843.

2. Jamie L McCall, et al. Pharmacol Res Perspect. 2024 Aug;12(4):e1230.

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