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KW 3902
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KW 3902图片
CAS NO:136199-02-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
KW 3902 (KW-3902) 是一种有效的选择性腺苷 A1 受体拮抗剂,正在开发用于治疗急性充血性心力衰竭和肾功能不全的患者。
Cas No.136199-02-5
别名1,3-二丙基-8-(3-正金刚烷基)黄嘌呤,KW-3902
化学名8-((2R,3as,5S,6as)-octahydro-2,5-methanopentalen-3a-yl)-1,3-dipropyl-1H-purine-2,6(3H,7H)-dione
Canonical SMILESO=C1N(CCC)C(N(CCC)C2=C1NC([C@@]3(C[C@H]4C5)[C@H]5C[C@H](C4)C3)=N2)=O
分子式C20H28N4O2
分子量356.46
溶解度DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 0.5 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450)[1].Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases[2].

References:
[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.