ARM1 (Synonyms: 4BSA) |
| رقم الكتالوجGC11201 |
ARM1 (4BSA) هو مثبط قوي لأمينوبيبتيداز وإيبوكسيد هيدرولازيُظهر ARM1 نشاطًا مثبطًا لأمينوبيبتيداز مع نشاط مثبط IC50 7.61 ميكرومتر وإيبوكسيد هيدرولاز مع IC50 12.4 ميكرومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 68729-05-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 68729-05-5 | SDF | |
| المرادفات | 4BSA | ||
| Chemical Name | 4-[4-(phenylmethyl)phenyl]-2-thiazolamine | ||
| Canonical SMILES | NC(N1)=SC=C1C(C=C2)=CC=C2CC3=CC=CC=C3 | ||
| Formula | C16H16N2S | M.Wt | 268.4 |
| الذوبان | ≤1mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7258 mL | 18.6289 mL | 37.2578 mL |
| 5 mM | 745.2 μL | 3.7258 mL | 7.4516 mL |
| 10 mM | 372.6 μL | 1.8629 mL | 3.7258 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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