LDN-212320
Based on 9 publication(s) in Google Scholar
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]
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 LDN-212320
More- Theranostics. 2024 Sep 3;14(14):5551-5570. [Abstract]
- Cell Death Dis. 2025 Jul 30;16(1):577. [Abstract]
- Arch Toxicol. 2025 Jun;99(6):2595-2609. [Abstract]
- Neural Regen Res. 2025 Jun 1;20(6):1721-1734. [Abstract]
- Neurobiol Dis. 2022 Dec:175:105922. [Abstract]
- Glia. 2023 May;71(5):1197-1216. [Abstract]
- PNAS Nexus. 2024 Aug 30;3(9):pgae362. [Abstract]
- Eur J Pain. 2019 Apr;23(4):765-783. [Abstract]
- Physiol Behav. 2025 Nov 1:301:115059. [Abstract]
生物活性
製品説明
IC50 & Target
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EAAT2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Astrocyte | EC50 |
1.8 μM
Compound: 45477
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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
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[PMID: 21875806] |
| Astrocyte | EC50 |
2.6 μM
Compound: 45477
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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
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[PMID: 21875806] |
体内実験
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.
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Animal Model:Mice[1].
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Dosage:10 or 20 mg/kg.
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Administration:IP 24 h before the injection of formalin.
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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 (F3, 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.
化学情報
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CAS 番号 894002-50-7
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性状 Solid
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分子量 293.39
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分子式 C17H15N3S
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Color White to gray
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SMILES
CC1=CC=CC=C1CSC2=NN=C(C3=NC=CC=C3)C=C2
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別名
LDN-0212320; OSU-0212320
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Theranostics
The m6A reader YTHDC2 promotes the pathophysiology of temporal lobe epilepsy by modulating SLC7A11-dependent glutamate dysregulation in astrocytes. [Abstract]2024 Sep 3;14(14):5551-5570. PMID: 39310099 -
Cell Death Dis
Astrocytic YAP prevents the glutamate neurotoxicity by upregulation of EAAT2 expression and promotes the gain of stemness in astrocytes in ischemic stroke mice. [Abstract]2025 Jul 30;16(1):577. PMID: 40739083 -
Arch Toxicol
Exposure to polystyrene nanoplastics causes anxiety and depressive-like behavior and down-regulates EAAT2 expression in mice. [Abstract]2025 Jun;99(6):2595-2609. PMID: 40019525 -
Neural Regen Res
Increased excitatory amino acid transporter 2 levels in basolateral amygdala astrocytes mediate chronic stress-induced anxiety-like behavior. [Abstract]2025 Jun 1;20(6):1721-1734. PMID: 39104111 -
Neurobiol Dis
Deficiency of astrocyte CysLT1R ameliorates depression-like behaviors in mice by modulating glutamate synaptic transmission. [Abstract]2022 Dec:175:105922. PMID: 36371059 -
Glia
Yes-associated protein regulates glutamate homeostasis through promoting the expression of excitatory amino acid transporter-2 in astrocytes via β-catenin signaling. [Abstract]2023 May;71(5):1197-1216. PMID: 36617748 -
PNAS Nexus
Exploring the role of spinal astrocytes in the onset of hyperalgesic priming signals in acid-induced chronic muscle pain. [Abstract]2024 Aug 30;3(9):pgae362. PMID: 39228816 -
Eur J Pain
Effects of glial glutamate transporter activator in formalin-induced pain behaviour in mice. [Abstract]2019 Apr;23(4):765-783. PMID: 30427564 -
Physiol Behav
Acupuncture waggle needling alleviates spastic movement disorder in post-stroke rats via GLT-1 activation to modulate Glu/GABA-Gln cycle. [Abstract]2025 Nov 1:301:115059. PMID: 40783057
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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
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.
| 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 関連分類
HY-12741 関連分類
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