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.
SC 57461A
目录号: GC18011纯度: >98%同义词: N-甲基-N-[3-[4-(苯甲基)苯氧基]丙基Β-丙氨酸盐酸盐
A potent, orally active inhibitor of LTA4 hydrolase
Cas No.: 423169-68-0
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥493.00 | 现货 | 1 | |
| 5mg | ¥1,679.00 | 现货 | 1 | |
| 10mg | ¥2,603.00 | 现货 | 1 | |
| 25mg | ¥5,867.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥952.00 | 现货 | 1 |
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产品描述 Description
产品文档 Product Documents
Purity:>98%
化学性质Chemical Properties
CAS 号
423169-68-0
同义词
N-甲基-N-[3-[4-(苯甲基)苯氧基]丙基Β-丙氨酸盐酸盐
化学名
3-[3-(4-benzylphenoxy)propyl-methylamino]propanoic acid;hydrochloride
SMILES
CN(CCCOC1=CC=C(C=C1)CC2=CC=CC=C2)CCC(=O)O.Cl
分子式
C20H25NO3.HCl
分子量
363.88 g/mol
溶解性
≥ 36.4mg/mL in DMSO
保存条件
Desiccate at 4°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
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