【KW 3902】KW 3902 CAS号:136199-02-5【结构式性质活性】-化源网

Rolofylline (KW-3902) 是一种有效的选择性 adenosine A1 receptor 拮抗剂,目前正在开发用于治疗急性充血性心力衰竭和肾功能损害的患者。Rolofylline 主要通过细胞色素 P450 (CYP450) 代谢为药理学活性的 M1-反式和 M1-顺式代谢物。Rolofylline 可以减轻突触前功能障碍,恢复体外神经元活动以及树突棘水平,可用于对抗Tau-诱导的神经退行性疾病相关的代谢减退以及神经功能障碍。

[ 描述 ]:

Rolofylline (KW-3902) 是一种有效的选择性 adenosine A1 receptor 拮抗剂,目前正在开发用于治疗急性充血性心力衰竭和肾功能损害的患者。Rolofylline 主要通过细胞色素 P450 (CYP450) 代谢为药理学活性的 M1-反式和 M1-顺式代谢物。Rolofylline 可以减轻突触前功能障碍,恢复体外神经元活动以及树突棘水平,可用于对抗Tau-诱导的神经退行性疾病相关的代谢减退以及神经功能障碍。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

[参考文献]

[1]. Stroh M, et al. Simultaneous pharmacokinetic model for rolofylline and both M1-trans and M1-cis metabolites. AAPS J. 2013 Apr;15(2):498-504.

[2]. Dennissen FJ, et al. Adenosine A1 receptor antagonist rolofylline alleviates axonopathy caused by human Tau ΔK280. Proc Natl Acad Sci U S A. 2016 Oct 11;113(41):11597-11602. Epub 2016 Sep 26.

[ 密度 ]:
1.262g/cm3

[ 沸点 ]:
578ºC at 760mmHg

[ 分子式 ]:
C₂₀H₂₈N₄O₂

[ 分子量 ]:
356.46200

[ 闪点 ]:
303.4ºC

[ 精确质量 ]:
356.22100

[ PSA ]:
72.68000

[ LogP ]:
2.78400

[ 蒸汽压 ]:
2.33E-13mmHg at 25°C

[ 折射率 ]:
1.605

详细MSDS(安全技术说明书)

[ 危害声明 ]:
H413

[ 危险品运输编码 ]:
NONH for all modes of transport

详细合成路线

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The effects of multiple doses of rolofylline on the single-dose pharmacokinetics of midazolam in healthy subjects.

Am. J. Ther. 17(1) , 53-60, (2010)

Rolofylline is a potent, selective adenosine A1 receptor antagonist that was under development for the treatment of patients with acute decompensated heart failure and renal function impairment. This ...

The disconnect between phase II and phase III trials of drugs for heart failure.

Nat. Rev. Cardiol. 10(2) , 85-97, (2013)

Hospitalization for heart failure (HF) is a clinical entity associated with high postdischarge morbidity and mortality, yet few therapies are available to improve outcomes in patients with this condit...

Design and rationale of the PROTECT study: a placebo-controlled randomized study of the selective A1 adenosine receptor antagonist rolofylline for patients hospitalized with acute decompensated heart failure and volume overload to assess treatment effect on congestion and renal function.

J. Card. Fail. 16(1) , 25-35, (2010)

Current treatment for acute decompensated heart failure (ADHF) is associated with incomplete resolution of symptoms and signs, recurrent symptoms of heart failure in-hospital and after discharge and h...

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公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Rolofylline

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥3749.0/10mg ￥16269.0/50mg ￥需询单/1g ￥需询单/1g

联系人：李先生

产品详情：KW 3902

公司名：上海阿拉丁生化科技股份有限公司