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LP-211
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。
LP-211图片
CAS NO:1052147-86-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 466.63
Formula C30H34N4O
CAS No. 1052147-86-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>100 mg/mL
Water:
Ethanol:
Chemical Name N-[(4-cyanophenyl)methyl]-6-[4-(2-phenylphenyl)piperazin-1-yl]hexanamide
Synonyms LP 211; LP211; LP-211
SMILES Code O=C(NCC1=CC=C(C#N)C=C1)CCCCCN2CCN(C3=CC=CC=C3C4=CC=CC=C4)CC2
实验参考方法
In Vitro

In vitro activity: LP-211 is a potent and selective 5-HT7 receptor agonist, with Ki of 0.58 nM, and is 324- and 245-fold more selective 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.


Kinase Assay: [3H]-labeled LSD was used for the binding assay at rat cloned 5-HT7 receptor. In 1 mL of incubation buffer (50 mM Tris, 10 mM MgCl2 and 0.5 mM EDTA, pH 7.4) are suspended 30 μg of membranes, 2.5 nM [3H]-LSD, LP-211 (6–9 concentrations). The samples are incubated for 60 min at 37°C. The incubation is stopped by rapid filtration on GF/A glass fiber filters (presoaked in 0.5% polyethylenimine for 30 min). The filters are washed with 3 × 53 mL of ice-cold buffer (50 mM Tris, pH 7.4). Nonspecific binding is determined in the presence of 10 μM 5-CT. Approximately 90% of specific binding is determined under these conditions


Cell Assay:

In Vivo LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in mice with mean Cmax 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.
Animal model Male adult Wistar rats (300-450 g)
Formulation & Dosage Dissolved in DMSO; 0.25 or 0.50 mg/kg; i.p
ReferencesJ Med Chem. 2008 Sep 25;51(18):5813-22; Am J Transl Res. 2016 Jun 15;8(6):2525-33; Synapse. 2017 Dec;71(12). doi: 10.1002/syn.21995.