Istradefylline

Pricing Availability   Qty
说明: Potent and selective A2A antagonist
别名: KW-6002
化学名: 8-[(1E)-2-(2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione
纯度: ≥99% (HPLC)
说明书
引用文献 (4)
评论 (1)
文献 (1)

生物活性 for Istradefylline

Istradefylline is a potent and selective adenosine A2A receptor antagonist (Ki values are 2.2 and 150 nM for A2A and A1 receptors respectively). Anticataleptic and antiparkinson agent; reverses drug-induced motor dysfunction in animal models.

技术数据 for Istradefylline

分子量 384.43
公式 C20H24N4O4
储存 Store at +4°C
纯度 ≥99% (HPLC)
CAS Number 155270-99-8
PubChem ID 5311037
InChI Key IQVRBWUUXZMOPW-PKNBQFBNSA-N
Smiles O=C1N(CC)C(C(N(C)C(/C=C/C3=CC(OC)=C(OC)C=C3)=N2)=C2N1CC)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Istradefylline

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 7.69 20

制备储备液 for Istradefylline

以下数据基于产品分子量 384.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.2 mM 13.01 mL 65.03 mL 130.06 mL
1 mM 2.6 mL 13.01 mL 26.01 mL
2 mM 1.3 mL 6.5 mL 13.01 mL
10 mM 0.26 mL 1.3 mL 2.6 mL

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产品说明书 for Istradefylline

分析证书/产品说明书
选择另一批次:

参考文献 for Istradefylline

参考文献是支持产品生物活性的出版物。

Shimada et al (1997) Adenosine A2A antagonists with potent anti-cataleptic activity. Bioorg.Med.Chem.Lett. 7 2349

Kanda et al (1998) Adenosine A2A receptors modify motor function in MPTP-treated common marmosets. Neuroreport 9 2857 PMID: 9760134

Shiozaki et al (1999) Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by rese. or MPTP. Psychopharmacology 147 90 PMID: 10591873


If you know of a relevant reference for Istradefylline, please let us know.

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查看全部 Adenosine A2A Receptor Antagonists

关键词: Istradefylline, Istradefylline supplier, Potent, selective, Adenosine, A2A, receptor, antagonists, KW-6002, KW6002, AA2AR, antiparkinsons, activity, antiparkinsonian, anticataleptics, Receptors, 5147, Tocris Bioscience

4 篇 Istradefylline 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Istradefylline 的部分引用包括:

John M et al (2021) Cannabis sativa terpenes are cannabimimetic and selectively enhance cannabinoid activity. Sci Rep 11 8232 PMID: 33859287

Cheng et al (2017) Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity. Structure 25 1275 PMID: 28712806

Orr et al (2018) Istradefylline reduces memory deficits in aging mice with amyloid pathology. Neurobiol Dis 110 29 PMID: 29100987

Wydra et al (2015) On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats. PLoS One 232 1767 PMID: 25420611


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Istradefylline 的评论

平均评分: 4 (Based on 1 Review.)

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Istradefylline on D2R antagonist induced motor impairment.
By Yunmin Ding on 12/07/2018
分析类型: In Vivo
种属: Mouse

i.p.

Istradefylline from Tocris worked wonderfully. At 3 mg/kg (in suspension in 8% Tween 80 in 0.9% saline), it reversed motor impairment induced by 0.16 mg/kg of the D2R antagonist eticlopride


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