TABLE 1

Activity of alanine-substituted MII analogs

Numbers in parentheses are 95% confidence intervals.

Toxin IC50
Rat α3β2 Rat α6/α3β2β3 Ratioa
nM
MII 2.18 (1.24-3.81) 0.39 (0.281-0.548) 5.59
MII[S4A] 15.8 (7.03-35.3) 0.733 (0.513-1.05) 21.56
MII[N5A] >10,000 793 (566-1110) >12.6
MII[P6A] 4,420 (1880-10,400) 253 (172-372) 17.5
MII[V7A] 4.46 (3.28-6.05) 10.6 (8.01-14.0) 0.421
MII[H9A] 59.0 (44.1-78.9) 0.790 (0.558-1.12) 74.7
MII[L10A] 1.47 (0.642-3.38) 0.482 (0.232-1.00) 3.05
MII[E11A] 8.72 (6.84-11.1) 0.160 (0.135-0.189) 54.5
MII[H12A] 4,660 (2420-9000) 604 (256-1420) 7.72
MII[S13A] 2.54 (1.92-3.35) 0.659 (0.450-0.966) 3.85
MII[N14A] 25.7 (17.0-38.9) 1.06 (0.742-1.52) 24.2
MII[L15A] 34.1 (19.4-59.9) 0.917 (0.657-1.28) 37.2
  • a IC50 α3β2/IC50 α6/α3/β2β3.