| Bioactivity | SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC50s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively[1]. |
| Invitro | SC-57461A inhibits ionophore-stimulated LTB4 production in whole blood with IC50s of 49, 166, and 466 nM in human mouse and rat, respectively[1].SC-57461A demonstrates excellent potency against LTA4 hydrolase (IC50=2.5 nM) and in whole cells (IC50=49 nM)[2]< |
| In Vivo | SC-57461A also shows excellent potency in the mouse ex vivo assay, inhibiting the production of LTB4 with an ED50=0.2 mg/kg and an ED90=1 mg/kg. SC-57461A also inhibits the production of LTB4 in the rat peritoneal model with an ED50=1 mg/kg[2]. SC-57461A is a potent, selective, and competitive inhibitor of LTA4 hydrolase with excellent activity in whole animals. SC-57461A demonstrates good oral activity in both the mouse and the rat[3]. Animal Model: |
| Name | SC-57461A |
| CAS | 423169-68-0 |
| Formula | C20H26ClNO3 |
| Molar Mass | 363.88 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Leslie J Askonas, et al. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A(4) hydrolase I: in vitro studies. J Pharmacol Exp Ther. 2002 F [2]. T D Penning. Inhibitors of leukotriene A4 (LTA4) hydrolase as potential anti-inflammatory agents. Curr Pharm Des. 2001 Feb;7(3):163-79. [3]. James F Kachur, et al. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A(4) hydrolase II: in vivo studies. J Pharmacol Exp Ther. 2002 Feb |