2. GPCR/G Protein Neuronal Signaling
  3. Melatonin Receptor
  4. Luzindole

Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.

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Luzindole Chemical Structure

Luzindole Chemical Structure

CAS No. : 117946-91-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 193 In-stock
Solution
10 mM * 1 mL in DMSO USD 193 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 120 In-stock
10 mg USD 181 In-stock
25 mg USD 330 In-stock
50 mg USD 470 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Luzindole Related Antibodies

Top Publications Citing Use of Products

View All Melatonin Receptor Isoform Specific Products:

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MT1 MT2

  • Biological Activity

  • Purity & Documentation

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Description

Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity[1][2][3].

IC50 & Target

MT2

 

Cellular Effect
Cell Line Type Value Description References
Melanophore IC50
2.1 μM
Compound: luzindole
Inhibitory concentration against melatonin-induced pigment aggregation by 50% in Xenopus laevis dermal melanophore cell line
Inhibitory concentration against melatonin-induced pigment aggregation by 50% in Xenopus laevis dermal melanophore cell line
[PMID: 9484496]
In Vitro

Luzindole (N-0774) (5-10 μg/ml) inhibits antigen-specific proliferation of the MBP-reactive LV-4 T cell line[1].

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

Luzindole Related Antibodies
In Vivo

Luzindole (N-0774) (30 mg/kg; i.p.; days 0-5) suppresses experimental autoimmune encephalomyelitis[2].
? Luzindole (N-0774) (30 mg/kg i.p.) reduces the time of immobility in a dose-dependent manner, the effect being more pronounced at midnight (60% reduction) than at noon (39% reduction). The effect of luzindole is time-dependent, showing a maximal effect at 60 min. The anti-immobility effect of luzindole (10 mg/kg i.p.) is prevented by the administration of melatonin (30 mg/kg i.p.). Luzindole (30 mg/kg i.p.) did not modify the time of immobility either at noon or midnight in the albino ND/4 mouse, or in the C57BL/6J mouse, which does not produce melatonin[3].

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

Animal Model: Twenty-three- to 12-week-old(SJL X PL/J ) F1 mice[2]
Dosage: 30 mg/kg
Administration: i.p.; days 0-5 (between 23: 00 and 1: 00 under conditions of minimal lighting)
Result: Effectively prevented experimental autoimmune encephalomyelitis.
Molecular Weight

292.37

Formula

C19H20N2O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(NCCC1=C(CC2=CC=CC=C2)NC3=C1C=CC=C3)=O
Shipping

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

DMSO : 100 mg/mL (342.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4203 mL 17.1016 mL 34.2032 mL
5 mM 0.6841 mL 3.4203 mL 6.8406 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
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Concentration
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Volume
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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 (8.55 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 (8.55 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: 100.0%

SDS (251 KB)

COA (254 KB)

Handling Instructions (2659 KB)
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
DMSO 1 mM 3.4203 mL 17.1016 mL 34.2032 mL 85.5081 mL
5 mM 0.6841 mL 3.4203 mL 6.8406 mL 17.1016 mL
10 mM 0.3420 mL 1.7102 mL 3.4203 mL 8.5508 mL
15 mM 0.2280 mL 1.1401 mL 2.2802 mL 5.7005 mL
20 mM 0.1710 mL 0.8551 mL 1.7102 mL 4.2754 mL
25 mM 0.1368 mL 0.6841 mL 1.3681 mL 3.4203 mL
30 mM 0.1140 mL 0.5701 mL 1.1401 mL 2.8503 mL
40 mM 0.0855 mL 0.4275 mL 0.8551 mL 2.1377 mL
50 mM 0.0684 mL 0.3420 mL 0.6841 mL 1.7102 mL
60 mM 0.0570 mL 0.2850 mL 0.5701 mL 1.4251 mL
80 mM 0.0428 mL 0.2138 mL 0.4275 mL 1.0689 mL
100 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8551 mL
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Luzindole 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:

Luzindole117946-91-5N-0774N0774N 0774Melatonin Receptorselectivepreferentiallyautoimmuneencephalomyelitisantidepressant-likesubtypeanti-immobilityInhibitorinhibitorinhibit

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