Luzindole (Synonyms: N-0774)

Name: Luzindole
Brand: MedChemExpress
SKU: HY-101254
Rating: 5.0 (18 reviews)

Cat. No.: HY-101254 Pureza: 99.53%: Ficha de datos
COA

SDS
Instrucciones de manejo
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Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel_1b) over MT1 (Mel_1a) with K_i 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 Estructura química

No. CAS : 117946-91-5

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	Obtener un presupuesto
200 mg	Obtener un presupuesto

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Revisión del cliente

Based on 18 publication(s) in Google Scholar

Other Forms of Luzindole:

Luzindole (Standard) Obtener un presupuesto

18 Publications Citing Use of MCE Luzindole

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Melatonin Receptor:

Ver todas las isoformas

MT1 MT2

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

MT2

Cellular Effect

Cell Line	Type	Value	Description	References
Melanophore	IC₅₀	2.1 3 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]
Melanophore	IC₅₀	2.1 3 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]
Melanophore	IC₅₀	2.1 3 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.

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.

Peso molecular

292.37

Fòrmula

C₁₉H₂₀N₂O

No. CAS

117946-91-5

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

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
10 mM	0.3420 mL	1.7102 mL	3.4203 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

Pureza y Documentación

Purity: 99.62%

Select Batch:

Ficha de datos (280 KB) SDS (254 KB)

COA (254 KB) HNMR (190 KB) LCMS (118 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Dubocovich ML, et al. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):365-75. [Content Brief]

[2]. Constantinescu CS, et al. Luzindole, a melatonin receptor antagonist, suppresses experimental autoimmune encephalomyelitis. Pathobiology. 1997;65(4):190-4. [Content Brief]

[3]. Dubocovich ML Antidepressant-like activity of the melatonin receptor antagonist, luzindole (N-0774), in the mouse behavioral despair test. Eur J Pharmacol. 1990 Jul 3;182(2):313-25. [Content Brief]

Complete Stock Solution Preparation Table

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

Luzindole Related Classifications

Neurological Disease

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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Luzindole (Synonyms: N-0774)

Revisión del cliente

Other Forms of Luzindole:

Luzindole Related Antibodies

18 Publications Citing Use of MCE Luzindole

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Melatonin Receptor:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Luzindole Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Luzindole Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report