Abstract: Prostate specific membrane antigen(PSMA) as a specific target antigen for prostate cancer has become an ideal target. The use of PSMA labeled with ⁶⁸Ga has become a hot topic in prostate cancer diagnosis, staging and efficacy evaluation. To develop a new ⁶⁸Ga labeled PSMA compound with better physical and chemical properties, a novel PSMA small molecule inhibitor ⁶⁸Ga-NOTA-ANCP-PSMA was designed, with 1-naphthylalanine, tranexamic acid and phenylalanine as the side chain. And its labeling method, physical and chemical properties and preliminary evaluation were carried out. ⁶⁸Ga was labeled to the PSMA compound directly, and the labeling conditions such as temperature, pH and precursor compound input amount were tested, respectively. The stability and octanol-water partition coefficient were determined, and the in vitro distribution of normal mice was determined. The labeling conditions should be controlled at pH=3.0-4.5, the labeling temperature was selected at 90.0-95.0 ℃, and the precursor compound concentration was not lower than 20 mg/L. In optimal labeling conditions, the labeling yield achieves to over 95%. The purified labeled compound shows good vitro stability, and radiochemical purity is stable in the PBS system and the serum protein system for 2 hours. The octanol-water partition coefficient is -1.36±0.01(n=3), which is a little higher than PSMA-617. The distribution in normal mice show that the compound clears fast in blood, mainly by kidney metabolism, lower uptake shows in non-target organs. The compound shows good properties, which is expected to be used for the diagnosis of prostate for PET, and provide a basis for developing prostate cancer theranostic targeted molecules probe for the future.