GIBH-130
Based on 3 publication(s) in Google Scholar
GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
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- Pureza: 99.62%
- No. CAS: 1252608-59-5
- Fòrmula: C20H20N6O
- Peso molecular:360.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) GIBH-130
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Actividad biológica
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IL-1β 3.4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BV-2 | IC50 |
3.4 nM
Compound: GIBH-130
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Antiinflammatory activity in LPS-stimulated mouse BV-2 cells assessed as inhibition of IL-1beta release at 10 uM and measured after 8 hrs by ELISA
Antiinflammatory activity in LPS-stimulated mouse BV-2 cells assessed as inhibition of IL-1beta release at 10 uM and measured after 8 hrs by ELISA
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[PMID: 35931005] |
GIBH-130 is a novel antineuroinflammatory agent that is identified through microglia-based phenotypic screenings. GIBH-130 (IC50 3.4 nM) is identified in screenings as one of the most effective inhibitors with an acceptable half-life. Pretreatment of microglia with GIBH-130 significantly reduces the production of these factors in response to Lipopolysaccharides (LPS) stimulation, and the extent of the reduction is dependent on the concentrations of GIBH-130. The IC50 values of GIBH-130 for NO and TNF-α inhibition are 46.24 and 40.82 μM, respectively. Notably, pretreatment with GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM). The inhibitory efficiency of GIBH-130 at 20 nM is comparable to 20 μM minocycline against IL-1β release. IL-1β is one of the major cytokines during neuroinflammatory progression of AD. So, it is meaningful to explain the selectivity of GIBH-130 against IL-1β (IC50 value 3.4 nM) over NO and TNF-α (IC50 value 46.24 and 40.82 μM, respectively) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1252608-59-5
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Appearance Solid
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Peso molecular 360.41
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Fòrmula C20H20N6O
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Color Off-white to pink
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SMILES
O=C(C1=NN=C(C2=CC=CC=C2)C=C1C)N3CCN(C4=NC=CC=N4)CC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Intestinal Klebsiella pneumoniae infection enhances susceptibility to epileptic seizure which can be reduced by microglia activation. [Abstract]2021 Jul 7;7(1):175. PMID: 34234109 -
Ecotoxicol Environ Saf
Factors ameliorate pro-inflammatory microglia polarization through inhibition of reactive astrocytes induced by 2-chloroethanol. [Abstract]2023 Aug:261:115130. PMID: 37311391 -
Solvente y solubilidad
DMSO : 50 mg/mL (138.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.94 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 (6.94 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.
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.
Protocolo
The murine microglial cell line N9 (N9 cells) are cultured in DMEM supplemented with 10% FBS, 1 mM sodium pyruvate, 100 U/mL penicillin, and 100 μg/mL streptomycin. All cultures are maintained in a humidified CO2 incubator at 37°C and 5% CO2. Stock N9 cells are passaged 2-3 times/week with a 1:4 split ratio and used within 8 passages. N9 cells (5×104 cells/well) are plated into 96-well microtiter plates, followed by the treatment of Minocycline (20 μM) or various concentrations of the GIBH-130 (25, 50, and 100 μM) for 18 h. The NO production is stimulated by incubation with LPS (1 μg/mL) for 48 h. The levels of NO in the culture medium are measured using the nitric oxide detection kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Sprague-Dawley (SD) rats (half male and half female, 250–270 g) are used. Rats exposed to Aβ25-35 received oral (p.o.) GIBH-130 (0.0022, 0.02, or 0.18 mg/kg), Donepezil hydrochloride (0.9 mg/kg), Memantine hydrochloride (1.8 mg/kg) or distilled water via gavage after the Aβ25-35 injection. The sham-operated group receive a p.o. administration of distilled water (n=10 per group). All compounds are systemically administered in a volume of 0.01 mL per g body weight once daily after the day of surgery until the end of the behavioral testing. The behavioral tests started 8 days after the Aβ25-35 injection and are performed sequentially.
Mice[1]
APP/PS1 transgenic mice (half male and half female, 14 weeks age) and age-and-strained-matched wild type mice (C57BL/6J) are used. APP/PS1 transgenic mice are randomly divided into six groups: model group, GIBH-130 0.0031, 0.028, and 0.25 mg/kg group, Donepezil hydrochloride 1.3 mg/kg group, and Memantine hydrochloride 2.6 mg/kg group (n=10 per group). C57BL/6J mice are used as normal control group (n=10). The doses of GIBH-130 and the positive drugs used in this mouse model are equivalent to the rat model. All mice receive oral administration at 15 weeks of age and continuously for 25 weeks until the end of the behavioral tests. The model group and normal control group receive the same volume of distilled water (0.01 mL per g body weight).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.7746 mL | 13.8731 mL | 27.7462 mL | 69.3654 mL |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | 13.8731 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 mL | 6.9365 mL | |
| 15 mM | 0.1850 mL | 0.9249 mL | 1.8497 mL | 4.6244 mL | |
| 20 mM | 0.1387 mL | 0.6937 mL | 1.3873 mL | 3.4683 mL | |
| 25 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7746 mL | |
| 30 mM | 0.0925 mL | 0.4624 mL | 0.9249 mL | 2.3122 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7341 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5549 mL | 1.3873 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1561 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8671 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.6937 mL |
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