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ARM1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ARM1图片
CAS NO:68729-05-5
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
ARM1 (4BSA) 是一种有效的氨肽酶和环氧化物水解酶抑制剂。 ARM1 显示氨肽酶抑制活性，IC50 为 7.61 μM，环氧化物水解酶抑制活性，IC50 为 12.4 μM。
Cas No.68729-05-5
别名4BSA
化学名4-[4-(phenylmethyl)phenyl]-2-thiazolamine
Canonical SMILESNC(N1)=SC=C1C(C=C2)=CC=C2CC3=CC=CC=C3
分子式C16H16N2S
分子量268.4
溶解度≤1mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ARM1 (4-(4-benzylphenyl) thiazol-2-amine) is a LTB4 synthesis inhibitor [1].

Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that catalyzes the synthesis of the proinflammatory mediator LTB4 from LTA4 and cleaves the chemotactic tripeptide Pro-Gly-Pro. LTB4 is a key lipid mediator in the innate immune response [1][2].

ARM1 is a LTB4 synthesis inhibitor. ARM1 is a thiazolamine that inhibits LTB4 synthesis and conversion of LTA4 to LTB4 by purified LTA4H with Ki value of 2.3 μM. 50- to 100-fold higher concentrations of ARM1 did not significantly affect hydrolysis of Pro-Gly-Pro by LTA4 hydrolase. In isolated human polymorphonuclear neutrophils (PMNs), ARM1 efficiently inhibited LTB4 synthesis with IC50 value of about 0.5 μM and complete inhibition at 5 μM. ARM1 inhibited the epoxide hydrolase activity of LTA4H without significantly affecting its ability to cleave Pro-Gly-Pro. In the crystal structure of LTA4H in complex with ARM1, ARM1 occupied the binding site for the ω-end of LTA4 [1].

References:
[1].  Stsiapanava A, Olsson U, Wan M, et al. Binding of Pro-Gly-Pro at the active site of leukotriene A4 hydrolase/aminopeptidase and development of an epoxide hydrolase selective inhibitor. Proc Natl Acad Sci U S A. 2014 Mar 18;111(11):4227-32.
[2].  Haeggstrm JZ. Leukotriene A4 hydrolase/aminopeptidase, the gatekeeper of chemotactic leukotriene B4 biosynthesis. J Biol Chem. 2004 Dec 3;279(49):50639-42.
[3].  Snelgrove RJ, Jackson PL, Hardison MT, et al. A critical role for LTA4H in limiting chronic pulmonary neutrophilic inflammation. Science. 2010 Oct 1;330(6000):90-4.