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 SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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. |
