YM-26734 is a competitive inhibitor of the secreted (Group II) form of phospholipase A2. The IC50 against rabbit platelet derived sPLA2 is 85 nM. YM-26734 is active against, but less potent for group I (pancreatic) sPLA2 (porcine pancreatic enzyme IC50 = 7 μM), and does not inhibit intracellular PLA2 isoforms.
Molecular Weight | 730.97 |
Formula | C45H62O8 |
CAS Number | 144337-18-8 |
Solubility (25°C) | DMSO: 20 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] V D Mouchlis, et al. The application of rational design on phospholipase A(2) inhibitors
[2] Rob C Oslund, et al. Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA
[3] U Tibes, et al. Phospholipase A2 inhibitors in development
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