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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAdelmidrolCat. No.: HY-B1026CAS No.: 1675-66-7分式: CHNO分量: 274.36作靶點: NF-B; COX; PPAR作通路: NF-B; Immunology/Inflammation; Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO :
2、34 mg/mL (123.92 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.6448 mL 18.2242 mL 36.4485 mL5 mM 0.7290 mL 3.6448 mL 7.2897 mL10 mM 0.3645 mL 1.8224 mL 3.6448 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Adelmidrol 發(fā)揮重的抗炎作,部分依
3、賴于 PPAR。Adelmidrol 降低 NF-B 易位,和 COX-2 表達。IC50 & Target NF-B COX-2 PPAR體外研究Adelmidrol is a palmitoylethanolamide analogue. Adelmidrol reduces NF-B translocation, COX-2, and p-ERK expression; proinflammatory cytokine release; and the incidence of nitrotyrosine and poly(ADP)ribose in1/2 Master of Small
4、 Molecules 您邊的抑制劑師www.MedChemEthe colon 1.體內(nèi)研究 Adelmidrol (10 mg/kg, o.s.) reduces significantly the degree and severity of the macroscopic and histologicsigns of colon injury. Moreover, 4 days after colitis induced by dinitrobenzene sulfonic acid (DNBS)treatment, all mice have diarrhea and a reduct
5、ion in body weight (compared with the sham groups).Adelmidrol (10 mg/kg, o.s.) treatment significantly reduces the loss of body weight. The inflammatory boweldisease (IBD) induced by DNBS intrarectally administered is also characterized by an augmentation inmyeloperoxidase (MPO) activity, an indicat
6、or of neutrophil accumulating in the colon. This is consistent withlight microscopic observations showing the colon of vehicle-treated DNBS mice to contain a large number ofneutrophils. In contrast, Adelmidrol (10 mg/kg, o.s.) significantly reduces the degree of polymorphonuclearcell infiltration (d
7、etermined as reduction in MPO activity) in inflamed colon 1.PROTOCOLAnimal Mice 1Administration 1 Male adult CD1 mice (25-30 g) and male mice (20-27 g) are placed in a controlled environment andmaintained on a 12-hour light/dark cycle with food and water available ad libitum. Mice are casually divid
8、edinto the following groups (10 in each group) (1)Sham+vehicle group: Vehicle solution (saline) is given by oraladministration for 4 days. (2) Sham+Adelmidrol (10 mg/kg): Administered o.s. for 4 days. (3) DNBS+vehicle:Mice are injected by DNBS as described, and vehicle (saline) is given o.s. each da
9、y for 4 days, starting 60minutes after the injection of DNBS. (4) DNBS+Adelmidrol (10 mg/kg): Mice are injected by DNBS asdescribed, and Adelmidrol (10 mg/kg) is given o.s. each day, starting 60 minutes after administration ofDNBS 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Cordaro M, et al. Adelmidrol, a Palmitoylethanolamide Analogue, as a New Pharmacological Treatment for the Management ofInflammatory Bowel Disease. Mol Pharmacol. 2016 Nov;90(5):549-561.McePdfHeightCaution: Product has not been fully validate
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