CM4620 is a selective Orai1 inhibitor, prevents Ca2+ entry in acinar cells. The intravenous administration of CM4620 reduces the severity of acute pancreatitis in the rat, a hitherto untested species. SOCE via STIM1/Orai complexes promotes activation and fibroinflammatory gene expression within pancreatic stellate cells. CM4620 also decreased myeloperoxidase activity and inflammatory cytokine expression in pancreas and lung tissues, fMLF peptide-induced oxidative burst in human neutrophils, and cytokine production in human peripheral blood mononuclear cells (PBMCs) and rodent PaSCs, indicating that Orai1/STIM1 channels participate in the inflammatory responses of these cell types during acute pancreatitis.
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Name | CM4620 |
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Iupac Chemical Name | N-(5-(6-chloro-2,2-difluorobenzo[d][1,3]dioxol-5-yl)pyrazin-2-yl)-2-fluoro-6-methylbenzamide |
Synonyms | CM-4620; CM 4620; CM4620; |
Molecular Formula | C19H11ClF3N3O3 |
Molecular Weight | 421.7602 |
Smile | O=C(NC1=NC=C(C2=C(Cl)C=C(OC(F)(F)O3)C3=C2)N=C1)C4=C(C)C=CC=C4F |
InChiKey | QQMKTHUGOQDEIL-UHFFFAOYSA-N |
InChi | InChI=1S/C19H11ClF3N3O3/c1-9-3-2-4-12(21)17(9)18(27)26-16-8-24-13(7-25-16)10-5-14-15(6-11(10)20)29-19(22,23)28-14/h2-8H,1H3,(H,25,26,27) |
CAS Number | 1713240-67-5 |
Related CAS |
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Formulation | Solid powder |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Solubility:Soluble in DMSO |
Solubility | Soluble in DMSO |
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Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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Waldron RT, Chen Y, Pham H, et al. The Orai Ca2+ channel inhibitor CM4620 targets both parenchymal and immune cells to reduce inflammation in experimental acute pancreatitis. J Physiol. 2019;597(12):3085–3105. doi:10.1113/JP277856