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AC 55541
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。
AC 55541图片
CAS NO:916170-19-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 518.36
Formula C25H20BrN5O3
CAS No. 916170-19-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 51 mg/mL
Water: <1 mg/mL
Ethanol: N/A
SMILES Code O=C1C2=CC=CC=C2C(C(NC(C3=CC=CC=C3)=O)C(N/N=C(C)/C4=CC=CC(Br)=C4)=O)=NN1
Synonyms AC-55541; AC 55541; AC55541
实验参考方法
In Vitro

In vitro activity: AC-55541 is an agonist of protease-activated receptor (PAR) 2. AC-55541 activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM. AC-55541 was well absorbed when administered intraperitoneally to rats, reaching micromolar peak plasma concentrations. AC-55541 was stable to metabolism by liver microsomes and maintained sustained exposure in rats, with elimination half-lives of 6.1 h. Intrapaw administration of AC-55541 or AC-264613 elicited robust and persistent thermal hyperalgesia and edema. Coadministration of either a tachykinin 1 (neurokinin 1) receptor antagonist or a transient receptor potential vanilloid (TRPV) 1 antagonist completely blocked these effects. Systemic administration of either AC-55541 or AC-264613 produced a similar degree of hyperalgesia as was observed when the compounds were administered locally.


Kinase Assay: Phosphatidylinositol (PI) hydrolysis assays were performed as follows. For PAR2 WT, HEK 293T cells were seeded at 10,000 cells/well in DMEM (Invitrogen) supplemented with 10% fetal calf serum, penicillin (100 U/ml), and streptomycin (100 mg/ml) in a 37°C humidified atmosphere containing 5% CO2. Eighteen hours later, the cells were transfected as described above with the indicated plasmid DNAs (30 ng/well of a 96-well plate). Approximately 20 to 24 h after transfection, the cells were washed and labeled overnight with DMEM culture medium containing 0.2 μCi of NET1114 (37 MBq/ml; PerkinElmer Life and Analytical Sciences, Waltham, MA) per well (0.1 ml).


Cell Assay: In brief, cells were plated 1 day before transfection using 7 × 103 cells in 0.1 ml of media per well of a 96-well plate. Cells were transiently transfected with 10 ng of receptor DNA and 30 ng of pSI-β-galactosidase (Promega) per well of a 96-well plate using Polyfect according to the manufacturer's instructions. One day after transfection, medium was changed, and cells were combined with ligands in DMEM supplemented with 25% Ultraculture synthetic supplement instead of calf serum to a final volume of 200 μl/well. After 5 days in culture, β-galactosidase levels were measured essentially as described. Cells were rinsed with phosphate-buffered saline (PBS), pH 7.4, before the addition of 200 μl of PBS supplemented with 3.5 mM O-nitrophenyl-β-d-galactopyranoside and 0.5% Nonidet P-40 (both Sigma-Aldrich). After incubation (2–4 h), the plates were read at 420 nm on a plate reader.

In Vivo Male Sprague-Dawley rats (Harlan (Indianapolis, IN), 150 to 200 g at the time of testing, were maintained in a climate-controlled room on a 12-h light/dark cycle (lights on at 7:00 AM), and food and water were available ad libitum. Rats were housed in pairs for at least 2 days before use. All of the testing was performed in accordance with the policies and recommendations of the International Association for the Study of Pain and the National Institutes of Health Guide for Care and Use of Laboratory Animals
Animal model Male Sprague-Dawley rats
Formulation & Dosage
References J Pharmacol Exp Ther. 2008 Dec;327(3):799-808.