Name | Zegocractin |
Description | Zegocractin (CM-4620) is an inhibitor of calcium-release activated calcium (CRAC) channels. |
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) [1]. |
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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : Insoluble DMSO : 100 mg/mL (237.10 mM)
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Keywords | Inhibitor | inhibit | CM 4620 | Calcium release-activated channels | Ca2+ release-activated Ca2+ channels | CRAC Channel | Zegocractin |
Inhibitors Related | Nisoldipine | Nimodipine | 2,5-Di-tert-butylhydroquinone | Diltiazem hydrochloride | Levetiracetam | L-Ascorbic acid | Lanthanum(III) chloride heptahydrate | Butamben | Ethyl cinnamate | 1-Octanol | 1,2,4-Trihydroxybenzene | Otilonium bromide |
Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |