F-15599 (Synonyms: NLX-101)
目录号: PL04966 纯度: ≥99%
CAS No. :635323-95-4
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中文名称
F-15599
英文名称
F-15599
英文别名
(3-chloro-4-fluorophenyl)-[4-fluoro-4-[[(5-methylpyrimidin-2-yl)methylamino]methyl]piperidin-1-yl]methanone;F-15599;(3-Chloro-4-fluorophenyl)-[4-fluoro-4-[[(5-methylpyrimidin-2-ylmethyl)amino]methyl]piperidin-1;4-Piperidinemethanamine, 1-(3-chloro-4-fluorobenzoyl)-4-fluoro-N-[(5-methyl-2-pyrimidinyl)methyl]- (9CI);83481Y1YCX;(3-Chloro-4-fluorophenyl)-(4-fluoro-4-(((5-methylpyrimidin-2-ylmethyl)amino)methyl)piperidin-1-yl)methanone;(3-Chloro-4-fluorophenyl)-[4-fluoro-4-[[(5-methylpyrimidin-2-ylmethyl)amino]methyl]piperidin-1-yl]methanone;F15599;GTPL3924;BCP31490;BDBM50476734;4-Piperidinemeth;(3-Chloro-4-fluorophenyl)(4-fluoro-4-((((5-methylpyrimidin-2-yl)methyl)amino)methyl)piperidin-1-yl)methanone
Cas No.
635323-95-4
分子式
C19H21ClF2N4O
分子量
394.85
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
F-15599 是一种高度选择性的 5-HT1A receptor 激动剂,Ki 值为 3.4 nM。
生物活性
F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K i of 3.4 nM.
性状
Solid
IC50 & Target[1][2]
5-HT1A Receptor 3.4 nM (Ki)
体内研究(In Vivo)
F15599 (0.06 or 0.12 mg/kg) significantly reduces l-DOPA-induced dyskinesia (LID), without affecting motor performance of rats. Rats treated with F15599 manifest less LID and mild 5-HT syndrome with the high dose of 30 μg/μL. F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, i,p,) results in a significant and dose-dependent (MED?=?0.125 mg/kg) delay in the latency to attack, and a potent reduction (ID 50 ?=?0.095 mg/kg) in the amount of aggressive behaviour directed towards the intruder rat. Starting from the 0.25 mg/kg dose, F15599 induces clear signs of the so-called serotonin syndrome characterized by flat body posture, head-waving, lower lip retraction and hindlimb abduction, leading to increased behavioural inactivity scores and social disengagement. F15599 increases the discharge rate of pyramidal neurones in medial prefrontal cortex (mPFC) from 0.2 μg/kg i.v and
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Meadows SM, et al. Characterizing the differential roles of striatal 5-HT1A auto- and hetero-receptors in the reduction of l-DOPA-induced dyskinesia. Exp Neurol. 2017 Jun;292:168-178.
[2]. de Boer SF, et al. Anti-aggressive effects of the selective high-efficacy biased 5-HT?A receptor agonists F15599 and F13714 in male WTG rats. Psychopharmacology (Berl). 2016 Mar;233(6):937-47.
溶解度数据
In Vitro: DMSO : 250 mg/mL (633.15 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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