貨號	規格	價格	上海	北京	武漢	南京
S81363-10mg	98.0%	￥140.00 S81363-10mg ￥140.00 現貨	9009 >10	-	-	-
S81363-50mg	98.0%	￥200.00 S81363-50mg ￥200.00 現貨	1808 >10	-	-	-
S81363-250mg	98.0%	￥600.00 S81363-250mg ￥600.00 現貨	365 >10	-	-	-
S81363-1g	98.0%	￥1350.00 S81363-1g ￥1350.00 現貨	99 >10	-	-	-

產品介紹

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.

產品描述：

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.

靶點：

Ki: 2.2 nM (adenosine A2A receptor);AdenosineReceptor

體內研究：

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

參考文獻：

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)

保存條件：

-20℃

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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