2. GPCR/G Protein
  3. Adenosine Receptor
  4. Istradefylline

Istradefylline  (Synonyms: 伊曲茶碱; KW-6002)

目录号: HY-10888 纯度: 99.70%
COA 产品使用指南

摩尔计算器

Istradefylline 是一种有效的，选择性的，可口服的 adenosine A2A receptor 拮抗剂，在帕金森疾病模型试验中，Ki 值为 2.2 nM。

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Istradefylline Chemical Structure

Istradefylline Chemical Structure

CAS No. : 155270-99-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥726
In-stock
1 mg ￥206
In-stock
5 mg ￥412
In-stock
10 mg ￥660
In-stock
25 mg ￥1056
In-stock
50 mg ￥1550
In-stock
100 mg ￥2450
In-stock
200 mg ￥3900
In-stock
500 mg ￥5900
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Istradefylline:

Istradefylline 相关抗体

Top Publications Citing Use of Products

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target

Ki: 2.2 nM (adenosine A2A receptor)
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
5250 nM
Compound: 2, KW 6002
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
[PMID: 23602401]
体外研究
(In Vitro)

Istradefylline has 70-fold greater affinity for the A2AR than the A1 receptor with Ki of 2.2 nM versus 150 nM[1]. Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes[4]. Istradefylline binds to A1 receptor, A2A receptor, and A3 receptor in human with Kis of >287 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 receptor and A2A receptor in mouse, respectively[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Istradefylline 相关抗体:
体内研究
(In Vivo)

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[1]. 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[2]. 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

384.43

Formula

C20H24N4O4
CAS 号
性状

固体

颜色

Off-white to yellow

中文名称

伊曲茶碱
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25.33 mg/mL (65.89 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6013 mL 13.0063 mL 26.0125 mL
5 mM 0.5203 mL 2.6013 mL 5.2025 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.41 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.70%

COA (193 KB) LCMS (112 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[5]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

The animals are housed either in pairs or alone under standard conditions at a temperature of 24-26°C and 50-60% relative humidity using a 12-h light-dark cycle. Diet consisted of standard food pellets, fresh fruit, and Mazuri marmoset jelly. The animals are treated with MPTP in a dose of 2.0 mg/kg sc daily for 5 days. Following MPTP treatment 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 Mazuri marmoset jelly and fresh fruit puree until they are able to maintain them-selves. Prior to behavioral testing, from 6-8 weeks to 8 months after exposure to MPTP, all animals show a marked reduction of basal locomotor 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-80 and 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.
参考文献

Istradefylline 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 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
15 mM 0.1734 mL 0.8671 mL 1.7342 mL 4.3354 mL
20 mM 0.1301 mL 0.6503 mL 1.3006 mL 3.2516 mL
25 mM 0.1041 mL 0.5203 mL 1.0405 mL 2.6013 mL
30 mM 0.0867 mL 0.4335 mL 0.8671 mL 2.1677 mL
40 mM 0.0650 mL 0.3252 mL 0.6503 mL 1.6258 mL
50 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3006 mL
60 mM 0.0434 mL 0.2168 mL 0.4335 mL 1.0839 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Istradefylline155270-99-8KW-6002伊曲茶碱KW6002KW 6002Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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