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KF-950 was investigated for in vitro spermicidal activity and as-sessed for inhibition ability of the proteolytic activity of acrosin by thegelatin substrate film method on rat spermatozoa. The results showedthe lowest spermicidal concentration was 1.56±0.13 mg/ml within 20seconds and 0.73 ± 0.07 mg/ml within 120 seconds, which is muchlower than that of NP-9( P < 0.01). KF-950 can inhibit the spermmean halo rate and diameter significantly. When the concentration ofKF-950 was 1×10~(-12) mg/ml, mean halo rate was 83.00±7.10% andmean halo diameter was 18.27 ± 1.94μm (Compared with the controlgroup, P <0.01). No halo presented when the concentration was 1×10~(-3) mg/ml. ED_(50) was 4.15×10~(-7) mg/ml on mean halo rate and 2.34×10~(-7) mg/ml on mean halo diameter. This study suggests that KF-950has strong effects on the acrosin proteolytic inhibition and weak effectson the spermicidal activity. KF-950 is a new acrosin inhibitor agent.(Reprod Contracep 2000; 20: 333-337)
KF-950 was investigated for in vitro spermicidal activity and as-sessed for inhibition ability of the proteolytic activity of acrosin by the gelatin substrate film method on rat spermatozoa. The results showed the lowest spermicidal concentration was 1.56 ± 0.13 mg / ml within 20 seconds and 0.73 ± 0.07 mg / ml within 120 seconds, which is muchlower than that of NP-9 (P <0.01). KF-950 can inhibit the sperm dilution and diameter significantly. When the concentration of KF-950 was 1 × 10-12 ) mg / ml, mean halo rate was 83.00 ± 7.10%, and methanole diameter was 18.27 ± 1.94 μm (Compared with the control group, P <0.01) No halo presented when the concentration was 1 × 10 -3 mg / ml (50) was 4.15 × 10 -7 mg / ml on mean halo rate and 2.34 × 10 -7 mg / ml on mean halo diameter. This study suggests that KF-950 has strong effects on the acrosin proteolytic inhibition and weak effects of the spermicidal activity. KF-950 is a new acrosin inhibitor agent. (Reprod Contracep 2000; 20: 333-337)