Methyl-ISP, a newly developed organophosphorous insecticide, is used in China to treat and protect plants from pest infestation. Our studies demonstrated that methyl-ISP is metabolized rapidly in rat and mouse. Its toxicity was low, no obvious accumulative toxicity, chronic toxicity, teratogenicity, mutagenicity, reproductive toxicity or delayed neurotoxicity could be observed. It is therefore concluded that methyl-ISP is relatively safe to animals and human subjects. methyl-ISP is now employed to replace the other commonly used insecticide hexachlorobenzene (666) in agriculture. A preliminary study was performed to elucidate the mechanism of intoxication at subcellular levels.