1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

LP-211 

目录号: HY-111455 纯度: 99.66%
产品使用指南

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)。

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LP-211 Chemical Structure

LP-211 Chemical Structure

CAS No. : 1052147-86-0

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥1089 In-stock
5 mg ¥990 In-stock
10 mg ¥1750 In-stock
25 mg ¥3800 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).

IC50 & Target

Ki: 0.58 nM (5-HT7 receptor), 188 nM (5-HT1A receptor), 142 nM (D2 receptor)[1]

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[1].

In Vivo

LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean Cmax of 0.76 ± 0.32 μg/mL at 30 min[1]. 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[2]. 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[3].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.1431 mL 10.7154 mL 21.4307 mL
5 mM 0.4286 mL 2.1431 mL 4.2861 mL
10 mM 0.2143 mL 1.0715 mL 2.1431 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

Binding of [3H]-LSD at rat cloned 5-HT7 receptor is performed in the assay. 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[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

LP-211 is formulated in 1% dimethyl sulfoxide (DMSO) in saline (0.9% NaCl)[3].

Rats[3]
Thirty male adult Wistar rats (300-450 g) are assessed for novelty preference behavior after acute treatment (administered immediately after the training session and 24 h before the test session). After a 4 weeks' wash out, the rPDT is conducted to evaluate attraction from a greater/uncertain reward, with a sub-chronic treatment (five injections, immediately after sessions which follow the indifferent point). Food restriction, imposed by the experimenter through a limited quantity of food given at the end of each rPDT session, is applied to increase motivation to work for food delivery. All behavioral tests take place between 9:30 am and 4:00 pm. Rats are randomly assigned to treatment (LP-211 at 0.25 or 0.50 mg/kg i.p.) and control groups (injection volume 10 mL/kg; n = 10 per group). The brain penetrant 5-HT7R agonist LP-211 is dissolved in a vehicle solution of 1% dimethyl sulfoxide (DMSO) in saline (0.9% NaCl). Control group receives the vehicle strictly in the same conditions[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

466.62

Formula

C₃₀H₃₄N₄O

CAS No.

1052147-86-0

SMILES

O=C(NCC1=CC=C(C#N)C=C1)CCCCCN2CCN(C3=CC=CC=C3C4=CC=CC=C4)CC2

Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 106.6 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.66%

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LP-211
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HY-111455
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