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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -Zegocractin
Zegocractin

Chemical Structure : Zegocractin

CAS No.: 1713240-67-5

Zegocractin (CM4620, CM-4620)

货号: PC-38432Not For Human Use, Lab Use Only.

Zegocractin (CM4620) is a selective small molecule CRAC (Orai1) channel inhibitor, inhibits Orai1/STIM1-mediated Ca2+ currents and Orai2/STIM1-mediated currents with IC50 of 120 nM and 900 nM, respectively.

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

生物&药学活性

Zegocractin (CM4620) is a selective small molecule CRAC (Orai1) channel inhibitor, inhibits Orai1/STIM1-mediated Ca2+ currents and Orai2/STIM1-mediated currents with IC50 of 120 nM and 900 nM, respectively.
CM4620 efficiently blocks store-operated Ca2+ entry (SOCE) in pancreatic acinar cells.
CM4620 prevents cell death and trypsinogen activation in primary rodent and human acini.
CM4620 administration (20 mg/kg) significantly reduces pancreatitis responses in mouse cerulein acute pancreatitis.
CM4620 inhibits CCK-induced NFAT and NF-κB activities in pancreatic acinar cells, inhibits cytokine production in PBMCs (IC50, 47 to 952 nM) and reduces oxidative burst in neutrophils.

物理化学性质&存储条件

分子量 421.760
分子式 C19H11ClF3N3O3
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-(5-(6-chloro-2,2-difluorobenzo[d][1,3]dioxol-5-yl)pyrazin-2-yl)-2-fluoro-6-methylbenzamide

参考文献

1. Waldron RT, et al. J Physiol. 2019 Jun;597(12):3085-3105.

2. Uchimura T, et al. Biomedicines. 2021 Oct 31;9(11):1589.

3. Gerasimenko JV, et al. Function (Oxf). 2022 Jan 31;3(2):zqac002.

4. Wen L, et al. Gastroenterology 149, 481-92.e7.

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