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Istradefylline 98%

Istradefylline

源叶(MedMol)
S81363
155270-99-8
C20H24N4O4
384.43
MFCD00928421
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S81363-10mg 98% ¥140.00元 >10 - - -
源叶(MedMol) S81363-50mg 98% ¥200.00元 >10 - - -
源叶(MedMol) S81363-250mg 98% ¥600.00元 >10 - - -
源叶(MedMol) S81363-1g 98% ¥1350.00元 >10 - - -
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产品介绍

Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
产品描述: Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
靶点: Ki: 2.2 nM (adenosine A2A receptor);AdenosineReceptor
体内研究:
Istradefylline (3.3 mg/kg, i.p.) treatment before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later. Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with an ED50 of 0.05 mg/kg and 0.26 mg/kg, respectively. Istradefylline is over 10 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-induced catalepsy. Istradefylline (10 mg/kg, p.o.) results an increase in locomotor activity to approximately twice that 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 on locomotor activity and improvement of motor disability but not dysKinesia
参考文献:
1. Chen JF, et al. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's 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 catalepsy and hypokinesia caused by reserpine 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 agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. 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 rat striatal 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 models of Parkinson's disease and cognition. J Pharm
溶解性: DMSO  :  25.33  mg/mL  (65.89  mM;  Need  ultrasonic  and  warming)
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.601 ml 13.006 ml 26.013 ml
5 mM 0.52 ml 2.601 ml 5.203 ml
10 mM 0.26 ml 1.301 ml 2.601 ml
50 mM 0.052 ml 0.26 ml 0.52 ml
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参考文献

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