LDN-212320 (Synonyms: LDN-0212320; OSU-0212320)

Name: LDN-212320
Brand: MedChemExpress
SKU: HY-12741
Rating: 5.0 (9 reviews)

Cat. No.: HY-12741 Pureza: 98.92%: Ficha de datos
COA

SDS
Instrucciones de manejo
FAQs
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LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC^[1]

Para uso exclusivo en investigación. No vendemos a pacientes.

LDN-212320 Estructura química

No. CAS : 894002-50-7

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
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
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	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE LDN-212320

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas EAAT:

Ver todas las isoformas

EAAT1 EAAT2 EAAT3 EAAT4 EAAT5

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

EAAT2

Cellular Effect

Cell Line	Type	Value	Description	References
Astrocyte	EC₅₀	2.6 3 Compound: 7-4	Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to beta-actin protein expression Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to beta-actin protein expression	[PMID: 21875806]
Astrocyte	EC₅₀	1.8 3 Compound: 7-4	Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to GAPDH protein expression Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to GAPDH protein expression	[PMID: 21875806]
Astrocyte	EC₅₀	1.8 3 Compound: 45477	Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to GAPDH protein expression Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to GAPDH protein expression	[PMID: 21875806]
Astrocyte	EC₅₀	1.8 3 Compound: 7-4	Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to GAPDH protein expression Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to GAPDH protein expression	[PMID: 21875806]
Astrocyte	EC₅₀	2.6 3 Compound: 45477	Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to beta-actin protein expression Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to beta-actin protein expression	[PMID: 21875806]
Astrocyte	EC₅₀	2.6 3 Compound: 7-4	Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to beta-actin protein expression Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to beta-actin protein expression	[PMID: 21875806]

In Vivo

LDN-212320 (10 or 20 mg/kg, i.p) significantly attenuates formalin-evoked nociceptive behavior^[1].
LDN-212320 (10 or 20 mg/kg, i.p) significantly reverses formalin-induced impaired hippocampal-dependent behavior. In addition, LDN-212320 (10 or 20 mg/kg, i.p) increases GLT-1 expressions in the hippocampus and ACC^[1].
LDN-212320 (20 mg/kg, i.p) significantly reduced formalin induced-ERK phosphorylation, a marker of nociception, in the hippocampus and ACC^[1].

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

Animal Model:	Mice^[1].
Dosage:	10 or 20 mg/kg.
Administration:	IP 24 h before the injection of formalin.
Result:	Significantly attenuated licking and biting behavior during both phases 1 and 2 in a dose-dependent manner compared to formalin-injected mice. Significantly (P < 0.01 or P < 0.001) reduced the licking and biting behavior. Significantly increased preference for the displaced object (F_{3, 13} = 28.03, P < 0.01) compared to formalin-injected mice. Significantly (P < 0.001) increased interaction time with the displaced object compared to formalin-injected mice.

Peso molecular

293.39

Fòrmula

C₁₇H₁₅N₃S

No. CAS

894002-50-7

Appearance

Solid

Color

White to gray

SMILES

CC1=CC=CC=C1CSC2=NN=C(C3=NC=CC=C3)C=C2

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (170.42 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	3.4084 mL	17.0422 mL	34.0843 mL
5 mM	0.6817 mL	3.4084 mL	6.8169 mL
10 mM	0.3408 mL	1.7042 mL	3.4084 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (8.52 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 (8.52 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)

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: 98.92%

Select Batch:

Ficha de datos (274 KB) SDS (393 KB)

COA (248 KB) HNMR (251 KB) LCMS (95 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Ghallab Alotaibi, et al. Effects of glial glutamate transporter activator in formalin-induced pain behaviour in mice. Eur J Pain. 2019 Apr;23(4):765-783. [Content Brief]

[2]. Xuechao Xing, et al. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5774-7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4084 mL	17.0422 mL	34.0843 mL	85.2108 mL
	5 mM	0.6817 mL	3.4084 mL	6.8169 mL	17.0422 mL
	10 mM	0.3408 mL	1.7042 mL	3.4084 mL	8.5211 mL
	15 mM	0.2272 mL	1.1361 mL	2.2723 mL	5.6807 mL
	20 mM	0.1704 mL	0.8521 mL	1.7042 mL	4.2605 mL
	25 mM	0.1363 mL	0.6817 mL	1.3634 mL	3.4084 mL
	30 mM	0.1136 mL	0.5681 mL	1.1361 mL	2.8404 mL
	40 mM	0.0852 mL	0.4261 mL	0.8521 mL	2.1303 mL
	50 mM	0.0682 mL	0.3408 mL	0.6817 mL	1.7042 mL
	60 mM	0.0568 mL	0.2840 mL	0.5681 mL	1.4202 mL
	80 mM	0.0426 mL	0.2130 mL	0.4261 mL	1.0651 mL
	100 mM	0.0341 mL	0.1704 mL	0.3408 mL	0.8521 mL

LDN-212320 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:

LDN-212320894002-50-7LDN-0212320 OSU-0212320LDN212320LDN 212320LDN0212320LDN 0212320OSU0212320OSU 0212320OSU-0212320EAATExcitatory amino acid transporter Glutamate transporter;Inhibitorinhibitorinhibit

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LDN-212320 (Synonyms: LDN-0212320; OSU-0212320)

Revisión del cliente

LDN-212320 Related Antibodies

9 Publications Citing Use of MCE LDN-212320

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas EAAT:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

LDN-212320 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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SAFETY DATA SHEET (SDS)

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