| Description | SC 57461A is a potent and specific leukotriene A4 hydrolase (LTA4H) inhibitor. |
| In vitro | 57461A is a potent competitive inhibitor of recombinant human LTA(4) hydrolase when either LTA(4) (IC(50) = 2.5 nM, K(i) = 23 nM) or peptide substrates (IC(50) = 27 nM) are used.?In human whole blood, the IC(50) for calcium ionophore-induced LTB(4) production was 49 nM, indicative of good cell penetration.?Whole blood production of the cyclooxygenase metabolite thromboxane B(2) was not affected.?SC-57461A was also active in several other species, including mouse, rat, dog, and rhesus monkey.?The data indicate that SC-57461A is a potent and selective inhibitor of LTA(4) hydrolase[2]. |
| Synonyms | N -甲基- N -[3 - [4 - (苯甲基)苯氧基]丙基Β-丙氨酸盐酸盐 |
| molecular weight | 363.9 |
| Molecular formula | C20H26ClNO3 |
| CAS | 423169-68-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (151.14 mM) |
| References | 1. Penning T D , Chandrakumar N S , Desai B N , et al. Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase[J]. Bioorganic & Medicinal Chemistry Letters, 2002, 12(23):3383-3386. 2. Kachur, J. F . 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]. Journal of Pharmacology & Experimental Therapeutics, 2002, 300(2):583-587. |