RO2959 monohydrochloride (C09-1167-448)

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC 50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC 50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathwaysIn VitroRO2959 inhibits Orai1 and Orai3 with IC 50 values of 25 nM and 530 nM, respectively. RO2959 blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC 50 value of 265 nM. RO2959 is a potent SOCE inhibitor that blocks an IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells stably expressing human Orai1 and Stim1, as well as SOCE in human primary CD4 + T cells triggered by either T cell receptor (TCR) stimulation or thapsigargin treatment. RO2959 completely inhibits cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction). MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:CRAC channel 402 nM (IC 50 ) Orai1/Stim1 channels 25 nM (IC 50 ) IL-2. Specifications and Purity: 99%. Molecular Formula: C21H20ClF2N5OS. Molecular Weight: 463.93. PubChem CID: 45274292. Isomeric SMILES: CC1=C(CN(CC1)C2=NC=C(S2)C)C3=CN=C(C=N3)NC(=O)C4=C(C=CC=C4F)F.Cl.