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Istradefylline

Istradefylline

产品编号 T6552   CAS 155270-99-8
别名: 伊曲茶碱, KW-6002

Istradefylline (KW-6002) 是选择性的可口服的腺苷 A2A 受体拮抗剂,可用于研究药物滥用、睡眠障碍、肝损伤、帕金森病和不安腿综合征等的治疗和基础科学的试验。

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Istradefylline Chemical Structure
Istradefylline, CAS 155270-99-8
规格 价格/CNY 货期 数量
5 mg ¥ 338 现货
10 mg ¥ 477 现货
25 mg ¥ 897 现货
50 mg ¥ 1,297 现货
1 mL * 10 mM (in DMSO) ¥ 397 现货
产品目录号及名称: Istradefylline (T6552)
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选择批次  
纯度: 98.57%
纯度: 98.18%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Istradefylline (KW-6002)(Ki of 2.2 nM) is a selective adenosine A2A receptor (A2AR) antagonist, which is under development in Phase 3 trails. It has been used in trials studying the treatment and basic science of Drug Abuse, Sleep Disorder, Hepatic Impairment, Parkinson's Disease, and Restless Legs Syndrome, among others.
靶点活性 Adenosine A2A receptor:2.2 nM(Ki)
体外活性 The affinity of Istradefylline for the A2AR is 70-fold greater than that for the A1 receptor with Ki of 2.2 nM versus 150 nM. [1] Exposure of primary rat striatal astrocytes to Istradefylline results in concentration-dependent abolition of bFGF induction of astrogliosis in vitro. [5] Binding affinities (Ki) of Istradefylline for A1 receptor, A2A receptor, and A3 receptor in human are >287 nM, 9.12 nM, and >681 nM, respectively, for A1 receptor and A2A receptor in rat 50.9 nM and 1.57 nM, respectively, and for A1 receptor and A2A receptor in mouse 105.02 nM and 1.87 nM, respectively. [6]
体内活性 Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with 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. Administration of Istradefylline in combination with L-dopa (50 mg/kg) exerts prominent effects on haloperidol-induced and reserpine-induced catalepsy. [2] Oral administration of Istradefylline at 10 mg/kg to MPTP-treated common marmosets produces an increase in locomotor activity to approximately twice that of control and improves motor disability. Administration of Istradefylline (10 mg/kg, po, 90 minutes before SKF80723/quinpirole/L-DOPA) in combination with SKF80723 (1 mg/kg, ip), quinpirole (0.06 mg/kg ip), or L-DOPA (2.5 mg/kg po) produces a significant additive effect on locomotor activity and improvement of motor disability but not dyskinesia. [3] In the MPTP mice model, Istradefylline significantly attenuates striatal dopamine depletion under various conditions. Pretreatment with Istradefylline (3.3 mg/kg, i.p.) before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later. [1] Oral administration of Istradefylline protects against the loss of nigral dopaminergic neuronal cells induced by 6-hydroxydopamine in rats, and prevents the functional loss of dopaminergic nerve terminals in the striatum and the ensuing gliosis caused by MPTP in mice. [4] Chronic Istradefylline treatment does not improve the reversal deficits in dopamine-depleted rats. [7] The tremulous jaw movements induced by pimozide are significantly reduced by co-administration of either Istradefylline or tropicamide. Pimozide-induced increases in ventrolateral striatal c-Fos expression are reduced by a behaviorally effective dose of Istradefylline, in contrast to tropicamide by which c-Fos expression in pimozide-treated rats is actually increased. [8]
细胞实验 A CHO cell line permanently expressing the human adenosine A1or A2A?receptor is cultured in α-MEM supplemented with 10% (v/v) fetal bovine serum, 50 U/mL penicillin, and 50 μg/mL streptomycin. Cells are grown at 37°C in an environment of 5% CO2. These cells are seeded on black 96-well assay plates at a density of 15,000 cells/well, and then they are cultured for 24 h.
别名 伊曲茶碱, KW-6002
分子量 384.43
分子式 C20H24N4O4
CAS No. 155270-99-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 7.7 mg/mL (20 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6013 mL 13.0063 mL 26.0125 mL 65.0313 mL
5 mM 0.5203 mL 2.6013 mL 5.2025 mL 13.0063 mL
10 mM 0.2601 mL 1.3006 mL 2.6013 mL 6.5031 mL
20 mM 0.1301 mL 0.6503 mL 1.3006 mL 3.2516 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Chen JF, et al. J Neurosci, 2001, 21(10), RC143. 2. Shiozaki S, et al. Psychopharmacology (Berl), 1999, 147(1), 90-95. 3. Kanda T, et al. Exp Neurol, 2000, 162(2), 321-327. 4. Ikeda K, et al. J Neurochem, 2002, 80(2), 262-270. 5. Brambilla R, et al. Glia, 2003, 43(2), 190-194.
A2B receptor antagonist 1 Derenofylline BAY-545 Inosine Tonapofylline GW-493838 PSB 0777 ammonium hydrate Apadenoson TFA

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 神经退行性疾病化合物库 抗癌临床化合物库 抗癌上市药物库 抗帕金森病化合物库 经典已知活性库 人代谢物化合物库 抗阿尔茨海默症化合物库 血脑屏障通透化合物库 抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Istradefylline 155270-99-8 GPCR/G Protein Neuroscience Adenosine Receptor KW 6002 P1 receptor Inhibitor inhibit KW6002 伊曲茶碱 KW-6002 inhibitor

 

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