计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
伊曲茶碱, 腺苷 A2a 受体拮抗剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Istradefylline(KW6002)是口服活性的腺苷A2A受体拮抗剂，Ki为2.2 nM。A selective A(2A) antagonist used to study parkinson’s disease in vitro
Information
Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with K i of 2.2 nM. Phase 3.
In vitro
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. Exposure of primary rat striatal astrocytes to Istradefylline results in concentration-dependent abolition of bFGF induction of astrogliosis in vitro. 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.
In vivo
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. 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. 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. 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. Chronic Istradefylline treatment does not improve the reversal deficits in dopamine-depleted rats. 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.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
英文别名
KW-6002 | (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-1H-purine-2,6(3H,7H)-dione
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Istradefylline
生化机理
Istradefylline (KW-6002) 是一种选择性腺苷 A2A 受体 (A2AR) 拮抗剂，Ki值为 2.2 nM。第 3 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
腺苷 A2a 受体拮抗剂
名称和识别符
EC号
803-302-8
分子类型
小分子
Isomeric SMILES
CCN1C2=C(C(=O)N(C1=O)CC)N(C(=N2)/C=C/C3=CC(=C(C=C3)OC)OC)C
分子量
384.43
Reaxy-Rn
7863435
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7863435&ln=
技术文档
高级数据
产品属性
| ALogP | 2.5 |
|---|
关联靶点（人）
ADORA2A
Tclin
腺苷受体A2a(Adenosine receptor A2a)
(17 活性数据)
ADORA2B
Tclin
腺苷受体A2b(Adenosine receptor A2b)
(1 活性数据)
MAOB
Tclin
胺氧化酶[含黄素]B(Amine oxidase [flavin-containing] B)
(1 活性数据)
ADORA1
Tclin
腺苷受体A1(Adenosine receptor A1)
(2 活性数据)
ADORA3
Tchem
腺苷受体A3(Adenosine receptor A3)
(1 活性数据)
化学和物理性质
熔点
193 °C
安全和危险性（GHS）
象形图
信号词
Danger
危险声明
H301: 吞咽会中毒
预防措施声明
P321: 特殊处理（请参阅此标签上的...）。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P316: 如果吞咽：立即寻求紧急医疗救助。
WGK Germany
3
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）