MY-1250

MY-1250 inhibits the release of mediators (histamine and slow-reacting substance of anaphylaxis) in passively sensitized human lung tissue fragments in a dose-dependent manner^[1].
MY-1250 (36 μM) induces a rapid, transient increase in intracellular cAMP levels in rat mast cells, which peaks at 20 s and returns to baseline within 2 min. It also induces a rapid decrease in intracellular ATP levels in rat mast cells, which reaches the lowest value at 20 s and returns to baseline within 2 min^[1].
MY-1250 (3.6×10^-9 M - 3.6×10^-4 M; 20 s preincubation, 8 min antigen incubation) inhibits antigen-induced histamine release from passively sensitized rat peritoneal mast cells in a dose-dependent manner, with an IC₅₀ of 0.3 μM^[2].
MY-1250 (3.6×10^-6 M - 3.6×10^-5 M; 20 s preincubation) dose-dependently inhibits the antigen-induced initial elevation of [Ca²⁺]ᵢ in passively sensitized rat peritoneal mast cells, with an IC₅₀ of 0.25 μM, and this effect is closely correlated with its inhibitory effect on histamine release^[2].
MY-1250 inhibits antigen-induced histamine and SRS-A release from rat peritoneal exudate cells in a dose-dependent manner, but pre-incubation with these cells abolishes its inhibitory effect^[3].
MY-1250 (2.5×10^-5 M; 1 min) induces concentration-dependent phosphorylation of the 78 kDa protein in purified rat peritoneal mast cells, with an IC₅₀ of 2.0×10^-7 M, and this phosphorylation is blocked by co-treatment with the calcium ionophore A23187^[4].
MY-1250 potently inhibits antigen-induced histamine release from rat peritoneal exudate cells, with an IC₅₀ of 1.2×10^-7 M, but does not inhibit histamine release from the aforementioned cells induced by calcium ionophore A23187^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.