LP-211

目录号: PL01914 纯度: ≥99%
LP-211 是一种选择性的,可透过血脑屏障的 5-HT7 受体激动剂,Ki 值为 0.58 nM,选择性高于 5-HT1A 受体 (Ki,188 nM) 和 D2 受体 (Ki,142 nM)。
CAS No. :1052147-86-0
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PL01914-5mg 5mg ¥647.00 请登录
PL01914-10mg 10mg ¥982.00 请登录
PL01914-50mg 50mg ¥3225.00 请登录
PL01914-100mg 100mg ¥4785.00 请登录
PL01914-200mg 200mg ¥6785.00 请登录
PL01914-500mg 500mg 询价 询价
PL01914-10mM*1mLinDMSO 10mM*1mLinDMSO ¥1414.00 请登录
PL01914-1 mL x 10 mM (in DMSO) ¥674.00 请登录
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中文名称
LP-211
英文名称
LP-211
英文别名
6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid 4-cyano-benzylamide;N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide;N-[(4-Cyanophenyl)methyl]-4-[1,1′-biphenyl]-2-yl-1-piperazinehexanamide;GS-9674;GS9674;PX-104Cilofexor 1052147-86-0;LP-211
Cas No.
1052147-86-0
分子式
C28H23Cl2N3O5
分子量
552.41
包装储存
Pure form -20°C 3 years;4°C 2 years
详情描述
LP-211 是一种选择性的,可透过血脑屏障的 5-HT7 受体激动剂,Ki 值为 0.58 nM,选择性高于 5-HT1A 受体 (Ki,188 nM) 和 D2 受体 (Ki,142 nM)。
产品详情
LP-211 是一种选择性的,可透过血脑屏障的 5-HT7 受体激动剂,Ki 值为 0.58 nM,选择性高于 5-HT1A 受体 (Ki,188 nM) 和 D2 受体 (Ki,142 nM)。
生物活性
LP-211 is a selective and blood?brain barrier penetrant 5-HT 7 receptor agonist, with a K i of 0.58 nM, with high selectivity over 5-HT 1A receptor (K i , 188 nM) and D 2 receptor (K i , 142 nM).
性状
Oil
IC50 & Target[1][2]
5-HT7 Receptor 0.58 nM (Ki) 5-HT1A Receptor
体外研究(In Vitro)
LP-211 is a selective 5-HT7 receptor agonist, with a Ki of 0.58 nM, 324- and 245-fold selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM). LP-211 shows agonist properties with an EC50 of 0.6 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean C max of 0.76 ± 0.32 μg/mL at 30 min. LP-211 (0.003-0.3 mg/kg, i.p.) significantly increases the micturition volume in a dose-dependent manner, and causes significant increases in voiding efficiency in spinal cord-injured (SCI) rats, and such effects can be completely reversed by SB-269970. LP-211 (0.25 and 0.50 mg/kg i.p.) improves consolidation of chamber-shape memory in rats, resulting in significant novelty-induced hyperactivity and recognition. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
参考文献
[1]. Leopoldo M, et al. Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. J Med Chem. 2008 Sep 25;51(18):5813-22.
[2]. Norouzi-Javidan A, et al. Effect of 5-HT7 receptor agonist, LP-211, on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33. eCollection 2016.
溶解度数据
In Vitro: DMSO : 100 mg/mL (214.31 mM; Need ultrasonic)Ethanol : 50 mg/mL (107.15 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Leopoldo M, et al. Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. J Med Chem. 2008 Sep 25;51(18):5813-22.
[2]. Norouzi-Javidan A, et al. Effect of 5-HT7 receptor agonist, LP-211, on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33. eCollection 2016.

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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