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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIstradefyllineCat. No.: HY-10888CAS No.: 155270-99-8Synonyms: KW-6002分式: CHNO分量: 384.43作靶點: Adenosine Receptor作通路: GPCR/G Protein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 : 25.33 mg/mL

2、(65.89 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6013 mL 13.0063 mL 26.0125 mL5 mM 0.5203 mL 2.6013 mL 5.2025 mL10 mM 0.2601 mL 1.3006 mL 2.6013 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 Istradefylline種有效的,選擇性的,可服的 adenosine A2A r

3、eceptor 拮抗劑,在帕森疾病模型試驗中,Ki 值為 2.2 nM。IC50 & Target Ki: 2.2 nM (adenosine A2A receptor)體外研究Istradefylline has 70-fold greater affinity for the A2AR than the A1 receptor with Ki of 2.2 nM versus 150 nM1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Istradefylline causes concentration-dependent abol

4、ition of bFGF induction of astrogliosis in primary ratstriatal astrocytes 4. Istradefylline binds to A1 receptor, A2A receptor, and A3 receptor in human with Kis of287 nM, 9.12 nM, and 681 nM, respectively, 50.9 nM and 1.57 nM for A1 receptor and A2A receptor in rat,105.02 nM and 1.87 nM for A1 rece

5、ptor and A2A receptor in mouse, respectively 5.體內(nèi)研究 Istradefylline (3.3 mg/kg, i.p.) treatment before a single dose of MPTP attenuates the partial dopamine andDOPAC depletions measured in striata 1 week later 1. Istradefylline reverses CGS21680-induced andreserpine-induced catalepsy with an ED50 of

6、0.05 mg/kg and 0.26 mg/kg, respectively. Istradefylline is over10 times as potent in these models compared to other adenosine antagonists and dopamine agonist drugs.Istradefylline combined with L-dopa cuases potent effects on haloperidol-induced and reserpine-inducedcatalepsy 2. Istradefylline (10 m

7、g/kg, p.o.) results an increase in locomotor activity to approximately twicethat of control and improves motor disability in MPTP-treated common marmosets. Istradefylline (10 mg/kg,p.o.) in combination with SKF80723, quinpirole, or L-DOPA produces a significant additive effect onlocomotor activity a

8、nd improvement of motor disability but not dysKinesia 3.PROTOCOLCell Assay 5 A CHO cell line permanently expressing the human adenosine A1or A2A receptor is cultured in -MEMsupplemented with 10% (v/v) fetal bovine serum, 50 U/mL penicillin, and 50 g/mL streptomycin. Cells aregrown at 37C in an envir

9、onment of 5% CO2. These cells are seeded on black 96-well assay plates at adensity of 15,000 cells/well, and then they are cultured for 24 h.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal The animals are housed either in pairs or alone under sta

10、ndard conditions at a temperature of 24-26C andAdministration 3 50-60% relative humidity using a 12-h light-dark cycle. Diet consisted of standard food pellets, fresh fruit, andMazuri marmoset jelly. The animals are treated with MPTP in a dose of 2.0 mg/kg sc daily for 5 days.Following MPTP treatmen

11、t the animals are allowed to recover from the acute effects over a period of some 6-8 weeks. During MPTP treatment and throughout the following weeks, the animals are hand-fed with Mazurimarmoset jelly and fresh fruit puree until they are able to maintain them-selves. Prior to behavioral testing,fro

12、m 6-8 weeks to 8 months after exposure to MPTP, all animals show a marked reduction of basallocomotor activity, slower and less coordinated movements, abnormal postures of some parts of the body,and reduced checKing movements and eye blinks. Istradefylline (KW-6002) is suspended in 0.3% Tween-80and

13、10% sucrose solution and administered in a final volume of 2.0 mL/kg body weight by oral gavage.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Neurochem. 2019 May 23.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 M

14、aster of Small Molecules 您邊的抑制劑師www.MedChemE1. Chen JF, et al. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinsons disease. J Neurosci.2001 May 15;21(10):RC143.2. Shiozaki S, et al. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catale

15、psy and hypokinesia caused byreserpine or MPTP. Psychopharmacology (Berl). 1999 Nov;147(1):90-5.3. Kanda T, et al. Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonistsincreases antiparkinsonian activity but not dyskinesia in MPTP-treated mon

16、keys. Exp Neurol. 2000 Apr;162(2):321-7.4. Brambilla R, et al. Blockade of A2A adenosine receptors prevents basic fibroblast growth factor-induced reactive astrogliosis in ratstriatal primary astrocytes. Glia. 2003 Aug;43(2):190-4.5. Mihara T, et al. Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-5-amino-3-(4-fluorophenyl)pyrazin-2-yl-1-isopropylpyridine-2(1H)-one (ASP5854), in mode

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