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Istradefylline

伊曲茶碱,KW-6002

Istradefylline(KW-6002)是一种腺苷A2A受体(A2AR)选择性拮抗剂，Ki为2.2 nM。

目录号
EY1344
EY1344
EY1344
EY1344
EY1344
纯度
99.17%
99.17%
99.17%
99.17%
99.17%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
180
380
630
1400
2200
售价
180
380
630
1400
2200
库存
现货
现货
现货
现货
现货
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  • 生物活性

    Istradefylline is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM.

  • 体外研究

  • 体内研究

    30% propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)

  • 激酶实验

  • 细胞实验

  • 动物实验

    10 mg/kg 口服饲喂

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Chen JF, et al. J Neurosci, 2001, 21(10), RC143.
    [2] Kanda et al (1998) Adenosine A2A receptors modify motor function in MPTP-treated common marmosets. Neuroreport 9 2857.
    [3] Shiozaki et al (1999) Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology 147 90.
    [4] Shimada et al (1997) Adenosine A2A antagonists with potent anti-cataleptic activity. Bioorg.Med.Chem.Lett. 7 2349.

    分子式
    C20H24N4O4    		 分子量
    384.43    		 CAS号
    155270-99-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    20 mM    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02256033 Hepatic Impairment Drug: Istradefylline Kyowa Hakko Kirin Pharma, Inc.|Kyowa Kirin Pharmaceutical Development, Inc. Phase 1 2014-08-01 2015-05-19
    NCT02174250 Parkinson's Disease Drug: Istradefylline 40 mg|Drug: Rifampin 300mg BID + istradefylline 40mg Day 8 only Kyowa Hakko Kirin Pharma, Inc.|Kyowa Kirin Pharmaceutical Development, Inc. Phase 1 2014-06-01 2015-09-02
    NCT01968031 Idiopathic Parkinson's Disease Drug: Istradefylline 40 mg|Drug: Istradefylline 20 mg|Drug: Placebo Kyowa Hakko Kirin Pharma, Inc.|Kyowa Hakko Kirin Co., Ltd|Kyowa Kirin Pharmaceutical Development, Inc. Phase 3 2013-10-01 2016-12-09
    NCT02610231 Idiopathic Parkinson's Disease Drug: Istradefylline 20 mg or 40 mg Kyowa Hakko Kirin Pharma, Inc.|Kyowa Hakko Kirin Co., Ltd|Kyowa Kirin Pharmaceutical Development, Inc. Phase 3 2015-12-01 2017-03-13
    NCT00199381 Parkinson's Disease Drug: Istradefylline Kyowa Kirin Pharmaceutical Development, Inc. Phase 3 2005-10-01 2013-10-29
    NCT00957203 Parkinson's Disease Drug: Istradefylline Kyowa Hakko Kirin Co., Ltd Phase 3 2009-10-01 2012-08-30
    NCT00455507 Parkinson's Disease Drug: Istradefylline|Drug: Istradefylline|Drug: Placebo Kyowa Hakko Kirin Co., Ltd Phase 2 2007-03-01 2012-08-28
    NCT00955526 Parkinson's Disease Drug: Istradefylline|Drug: Istradefylline|Drug: Placebo Kyowa Hakko Kirin Co., Ltd Phase 3 2009-07-01 2012-08-28
    NCT00250393 Parkinson's Disease Drug: Istradefylline (KW-6002) Kyowa Hakko Kirin Co., Ltd Phase 2 2005-11-01 2012-08-28
    NCT00199420 Parkinson's Disease Drug: Istradefylline (KW-6002) Kyowa Kirin Pharmaceutical Development, Inc. Phase 3 2004-07-01 2016-07-12
    NCT00199355 Parkinson's Disease Drug: Istradefylline (KW-6002) Kyowa Hakko Kirin Co., Ltd Phase 2 2005-04-01 2014-05-21
    NCT00199407 Parkinson's Disease Drug: Istradefylline (KW-6002) Kyowa Kirin Pharmaceutical Development, Inc. Phase 3 2004-06-01 2016-07-12
    NCT00203957 Parkinson's Disease Drug: Istradefylline|Drug: Istradefylline University of Chicago Phase 3 2005-03-01 2013-06-10
    NCT00955045 Parkinson's Disease Drug: istradefylline Kyowa Kirin Pharmaceutical Development, Inc. Phase 2|Phase 3 2002-08-01 2016-07-12
    NCT00456586 Parkinson's Disease Drug: KW-6002 (istradefylline) Kyowa Kirin Pharmaceutical Development, Inc. Phase 2 2002-04-01 2016-07-12
    NCT02609477 Drug Abuse Drug: Istradefylline|Drug: Phentermine 45 mg|Other: Placebo Kyowa Hakko Kirin Pharma, Inc.|Kyowa Hakko Kirin Co., Ltd|Kyowa Kirin Pharmaceutical Development, Inc. Phase 1 2016-01-01 2016-08-17
    NCT00199446 Sleep Disorder|Restless Legs Syndrome Drug: Istradefylline (KW-6002) Kyowa Kirin Pharmaceutical Development, Inc. Phase 2 2005-07-01 2016-07-12
    NCT00199433 Parkinson's Disease|Movement Disorder Syndrome Drug: Istradefylline (KW-6002) Kyowa Kirin Pharmaceutical Development, Inc. Phase 2 2005-05-01 2016-07-12
    NCT00199394 Parkinson's Disease Drug: Istradefylline (KW-6002) Kyowa Hakko Kirin UK, Ltd.|Kyowa Kirin Pharmaceutical Development, Inc. Phase 3 2004-11-01 2016-07-12
    NCT00199368 Parkinson's Disease Drug: Istradefylline ( KW-6002) Kyowa Kirin Pharmaceutical Development, Inc.|Kyowa Hakko Kirin UK, Ltd. Phase 3 2004-10-01 2016-07-12
    NCT00456794 Parkinson's Disease Drug: Istradefylline (KW-6002) Kyowa Kirin Pharmaceutical Development, Inc. Phase 2 2002-03-01 2016-07-13
    NCT00006337 Parkinson's Disease Drug: KW-6002|Drug: IV Levodopa National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC) Phase 2 2000-10-01 2008-03-03

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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