The present invention is comprised of culturing microorganism having ability to produce FKI-1033 substance represented by the formula: ##STR00001## in a medium, accumulating FKI-1033 substance in the cultured medium, and isolating FKI-1033 substance from the cultured mass. The thus obtained FKI-1033 substance has ryanodine binding inhibition activity, insecticidal activity and anthelmintic activity, and is expected as useful drugs as agrochemicals, veterinary drugs and medicaments in effectiveness and toxicity.