Compound | Ca2+ Mobilization EC50 and Efficacy | Chemotaxis EC50 | ||||
---|---|---|---|---|---|---|
FPR1 | FPR2 | PMN | ||||
RBL-2H3 Cells | HL-60 Cells | RBL-2H3 Cells | HL-60 Cells | |||
μM (%) | μM | |||||
AG-09/1 | 2.4 ± 0.9 (140) | 3.4 ± 1.1 (120) | N.A. | N.A. | 0.4 ± 0.1 (130) | 0.9 ± 0.3 |
AG-09/2 | 15.8 ± 4.2 (110) | 21.5 ± 5.2 (120) | N.A. | N.A. | 5.8 ± 1.7 (105) | 5.8 ± 2.1 |
AG-26 | N.A. | N.A. | 0.5 ± 0.2 (85) | 0.4 ± 0.1 (70) | 0.7 ± 0.2 (95) | 12.6 ± 3.7 |
AG-09/3 | N.A. | N.A. | 9.9 ± 3.4 (105) | 19.3 ± 5.0 (95) | 10.4 ± 2.3 (105) | 0.3 ± 0.1 |
AG-09/4 | N.A. | N.A. | 7.7 ± 2.1 (105) | 15.1 ± 4.7 (90) | 16.4 ± 3.2 (75) | 5.3 ± 1.7 |
AG-09/5 | N.A. | N.A. | 12.6 ± 3.6 (125) | 2.7 ± 0.9 (70) | 7.0 ± 2.9 (85) | 1.5 ± 0.7 |
AG-09/6 | N.A. | N.A. | 9.7 ± 2.7 (80) | 5.0 ± 1.7 (75) | 28.8 ± 6.6 (55) | 4.7 ± 1.4 |
AG-09/7 | N.A. | N.A. | 5.4 ± 1.8 (75) | 5.8 ± 1.9 (80) | 10.8 ± 3.0 (35) | 0.9 ± 0.3 |
AG-09/8 | N.A. | N.A. | 0.3 ± 0.1 (145) | 14.8 ± 4.3 (50) | 1.4 ± 0.3 (125) | 2.2 ± 0.9 |
AG-09/9 | 10.7 ± 2.7 (45) | 17.7 ± 4.6 (25) | 10.8 ± 2.4 (45) | 9.6 ± 2.8 (125) | 8.2 ± 2.4 (90) | 4.2 ± 1.5 |
AG-09/10 | 18.6 ± 4.8 (80) | 14.3 ± 3.6 (65) | 11.1 ± 2.9 (80) | 6.9 ± 1.7 (40) | 1.9 ± 0.8 (100) | 0.3 ± 0.1 |
AG-22 | 19.7 ± 5.3 (55) | 11.1 ± 3.3 (40) | 15.0 ± 4.3 (60) | 17.2 ± 4.3 (70) | 23.6 ± 3.1 (85) | 9.6 ± 3.5 |
PMN, polymorphonuclear leukocytes; N.A., very low response (efficacy <20% of positive control) or no activity (no Ca2+ flux response was observed during the 3 min after addition of compounds under investigation).