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My CartCAS：155270-99-8
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Off-white to yellow Solid
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| CAS | 155270-99-8 |
| Name | Istradefylline |
| Molecular Formula | C20H24N4O4 |
| Molecular Weight | 384.43 |
| Solubility | Soluble in DMSO ≥1mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Off-white to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00928421 |
| SMILES | O=C1C2=C(N=C(/C=C/C3=CC(OC)=C(OC)C=C3)N2C)N(CC)C(N1CC)=O |
| Target Point | Adenosine Receptor |
| Passage | GPCR & G Protein |
| Background | Istradefylline is a potent and selective adenosine A2A receptor antagonist. |
| Biological Activity | 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。[1-5] |
| In Vitro | Istradefylline对A2AR的亲和力比A1受体高70倍，Ki为2.2 nM，而150 nM [1]。 Istradefylline导致原代大鼠纹状体星形胶质细胞中bFGF诱导星形胶质细胞增生的浓度依赖性消除[4]。 Istradefylline与人类A1受体，A2A受体和A3受体结合，Kis> 287 nM，9.12 nM，> 681 nM，大鼠的A1受体和A2A受体分别为50.9 nM和1.57 nM，105.02 nM和1.87 nM分别为小鼠的A1受体和A2A受体[5]。 |
| In Vivo | 在单剂量MPTP之前，Istradefylline(3.3 mg / kg，ip)治疗减弱1周后在纹状体中测量的部分多巴胺和DOPAC消耗[1]。 Istradefylline可逆转CGS21680诱导的和利血平诱导的强直性昏厥，ED50分别为0.05 mg / kg和0.26 mg / kg。与其他腺苷拮抗剂和多巴胺激动剂药物相比，Istradefylline在这些模型中的效力超过10倍。 Istradefylline联合L-dopa可对氟哌啶醇诱导和利血平诱导的强直性昏厥有潜在作用[2]。 Istradefylline(10 mg / kg，po)导致运动活性增加至对照的约两倍，并改善MPTP处理的普通mar猴的运动功能障碍。 Istradefylline(10 mg / kg，po)与SKF80723，喹吡罗或L-DOPA联合使用可对运动活动和运动功能障碍的改善产生显著的累加效应，但不会导致运动障碍[3]。 |
| Cell Experiment | 永久表达人腺苷A1或A2A受体的CHO细胞系在补充有10％(v / v)胎牛血清，50U / mL青霉素和50μg/ mL链霉素的α-MEM中培养。细胞在37℃，5％CO 2的环境中生长。将这些细胞以15，000个细胞/孔的密度接种在黑色96孔测定板上，然后培养24小时。 |
| Animal Experiment | 在标准条件下，在24-26℃和50-60％相对湿度的温度下，使用12小时光暗循环，将动物成对或单独饲养。饮食包括标准食物颗粒，新鲜水果和Mazuri Marmoset果冻。用MPTP以每天2.0mg / kg sc的剂量处理动物5天。在MPTP处理后，允许动物在约6-8周的时间内从急性效应中恢复。在MPTP治疗期间以及随后的几周内，动物用Mazuri mar猴果冻和新鲜水果泥手工喂养，直到它们能够维持它们自身为止。在进行行为测试之前，暴露于MPTP后6-8周至8个月，所有动物均表现出基础运动活动明显减少，运动速度减慢且协调性较差，身体某些部位姿势异常，以及减少的checKing运动和眼睛闪烁。将Istradefylline(KW-6002)悬浮于0.3％吐温-80和10％蔗糖溶液中，并通过口服强饲法以2.0mL / kg体重的最终体积给药。 |
| Data Literature Source | [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 |
| Unit | Bottle |
| Specification | 5mg 10mg |
是一种有效的，选择性的 adenosine A2A receptor 拮抗剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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