SC-57461A is a selective inhibitor of human recombinant LTB4 with IC50 value of 49 nM [1].
LTB4 (leukotriene B (4)) is a leukotriene and plays an important role in inflammation. LTB4 functions through interacting with the specific cell-surface receptors BLTR1 and BLTR2 [2].
SC-57461A is a potent LTB4 inhibitor and has a more potent activity than the reported LTA4 inhibitor RP64966. When tested with PMN cells, administration of SC-57461A significantly inhibited the synthesis of LT that induced by fMLP and PAF by acting on LTB4-BLTR1 interaction [3].
In fasted CD rat model of calcium ionophore A23187-induced eicosanoid production, oral administration of SC-57461A showed effective inhibition on LTB4 with ED50 value of 0.3-1.0 mg/kg. When tested with AA-induced edema on the ear, oral administration of SC-57461A resulted in markedly inhibition of edema at doses of 0.8, 4 and 20 mg/kg [1].
It is also been reported that SC-57461A inhibited LTB4A with Ki values of 23 nM and 27 nM for epoxide hydrolase and aminopeptidase, respectively [1].
References:
[1]. Kachur, J.F., 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. 300(2): p. 583-7.
[2]. Filgueiras, L.R., et al., Leukotriene B4-mediated sterile inflammation promotes susceptibility to sepsis in a mouse model of type 1 diabetes. Sci Signal, 2015. 8(361): p. ra10.
[3]. Grenier, S., et al., Arachidonic acid activates phospholipase D in human neutrophils; essential role of endogenous leukotriene B4 and inhibition by adenosine A2A receptor engagement. J Leukoc Biol, 2003. 73(4): p. 530-9.
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Chemical Properties
CAS No.
423169-68-0
Chemical Name
3-[3-(4-benzylphenoxy)propyl-methylamino]propanoic acid;hydrochloride
SMILES
CN(CCCOC1=CC=C(C=C1)CC2=CC=CC=C2)CCC(=O)O.Cl
Molecular Formula
C20H25NO3.HCl
Molecular Weight
363.88
Solubility
≥ 36.4mg/mL in DMSO
Storage
Desiccate at 4°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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