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Zegocractin

Chemical Structure : Zegocractin

CAS No.: 1713240-67-5

Zegocractin (CM4620, CM-4620)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 421.760
Formula C19H11ClF3N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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