Zegocractin

SKU: orb1296255

Description

Zegocractin (CM-4620) is a selective inhibitor of CRAC (Calcium Release-Activated Calcium) channels. It is a valuable research tool for studying calcium signaling in immune cells and has been utilized in both in vitro and in vivo models of inflammation and pancreatitis.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1713240-67-5
• MW: 421.76
• Purity: 99.59% (May vary between batches)
• Formula: C₁₉H₁₁ClF₃N₃O₃
• SMILES: Cc1cccc(F)c1C(=O)Nc1cnc(cn1)-c1cc2OC(F)(F)Oc2cc1Cl
• Target: Calcium Channel
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (7.82 mM);H2O:Insoluble;DMSO:140 mg/mL (331.94 mM)

Bioactivity

• Target IC50:
  Orai2/STIM1:119 nM|Orai2/STIM1:895 nM
• In Vivo:
  Mouse PACs are treated with CRAC inhibitors GSK-7975A or CM-4620 and monitored for their rate of Calcium uptake. Both CRAC inhibitors reduce the rate of store-operated Calcium entry into the ER to 50% of control levels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of the reuptake at 10 mM.
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• In Vitro:
  CM-4620 (compound 1) is more potent on Orai1 than Orai2-type CRAC channels. In human PBMCs, CM-4620 potently inhibits release of multiple cytokines which play important roles in T cells (IC50s, IFN γ: 138 nM, IL-6: 135 nM, IL-4: 879 nM, IL-1β: 240 nM, IL-10: 303 nM, IL-2: 59 nM, TNFα: 225 nM, IL-17 120 nM) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

N-(5-(6-Chloro-2,2-difluorobenzo[d][1,3]dioxol-5-yl)pyrazin-2-yl)-2-fluoro-6-methylbenzamide, Orai1/STIM1, Orai2/STIM1, inhibit, Inhibitor, Ca2+ release-activated Ca2+ channels, Calcium Channel, Calcium release-activated channels, CM 4620, CalciumChannel, CM4620, CM-4620, CRAC Channel, Zegocractin

Compound Identifiers

PubChem CID

122507647