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ARM1

Catalog No.
C4323
LTB4 synthesis inhibitor
Grouped product items
SizePriceStock Qty
5mg
$68.00
Ship with 5-10 days
10mg
$129.00
Ship with 5-10 days
50mg
$543.00
Ship with 5-10 days
100mg
$950.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt268.4
Cas No.68729-05-5
FormulaC16H16N2S
Solubility≤1mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide
Chemical Name4-[4-(phenylmethyl)phenyl]-2-thiazolamine
SDFDownload SDF
Canonical SMILESNC(N1)=SC=C1C(C=C2)=CC=C2CC3=CC=CC=C3
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

ARM1