2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. LP-211

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).

For research use only. We do not sell to patients.

LP-211 Chemical Structure

LP-211 Chemical Structure

CAS No. : 1052147-86-0

Size Price Stock Quantity
Oil + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Oil
5 mg USD 80 In-stock
10 mg USD 130 In-stock
50 mg USD 390 In-stock
100 mg USD 620 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

LP-211 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LP-211

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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

5-HT7 Receptor

0.58 nM (Ki)

5-HT1A Receptor

188 nM (Ki)

D2 Receptor

142 nM (Ki)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LP-211 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

466.62

Formula

C30H34N4O
CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (107.15 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.61%

COA (244 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References
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]

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.1431 mL 10.7154 mL 21.4307 mL 53.5768 mL
5 mM 0.4286 mL 2.1431 mL 4.2861 mL 10.7154 mL
10 mM 0.2143 mL 1.0715 mL 2.1431 mL 5.3577 mL
15 mM 0.1429 mL 0.7144 mL 1.4287 mL 3.5718 mL
20 mM 0.1072 mL 0.5358 mL 1.0715 mL 2.6788 mL
25 mM 0.0857 mL 0.4286 mL 0.8572 mL 2.1431 mL
30 mM 0.0714 mL 0.3572 mL 0.7144 mL 1.7859 mL
40 mM 0.0536 mL 0.2679 mL 0.5358 mL 1.3394 mL
50 mM 0.0429 mL 0.2143 mL 0.4286 mL 1.0715 mL
60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8929 mL
80 mM 0.0268 mL 0.1339 mL 0.2679 mL 0.6697 mL
100 mM 0.0214 mL 0.1072 mL 0.2143 mL 0.5358 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

LP-211 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LP-2111052147-86-0LP211LP 2115-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LP-211
Cat. No.:
HY-111455
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.