Application

Synta66 has been used:as a Ca²⁺release-activated calcium (CRAC) channel inhibitor to study its effects on ORAI isoformsas an ORAI1 blocker to study its effects on the entry of Ca²⁺ in chronic lymphocytic leukemia (CLL) B cellsas a CRAC blocker to study its effects on the influx of Ca²⁺ by store-operated Ca²⁺entry (SOCE) in enamel cells

Biochem/physiol Actions

Synta66 (S66) is a CRAC (Ca2+ release-activated Ca2+) channel inhibitor that blocks SOCE (store-operated Ca2+ entry) upon Ca2+ depletion from intracellular stores by thapsigargin in human vascular smooth muscle cells (VSMCs) with high potency (IC50 = 26 nM & 43 nM based on maximum Ca2+ level & rate of increase, respectly). Synta66 exhibits no affinity toward a range of receptors and ion channels (e.g. L-type Ca2+ channel) and does not affect TRPC1/5-mediated SOCE or store-operated non-selective cationic current. Leukocytes are reported to be less sensitive to CRAC inhibition by Synta66 (IC50 = 1.76 µM/HL-60, 1 ?M/Jurkat, 1.4 µM/rat RBL).