L6H21
Based on 1 publication(s) in Google Scholar
L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.
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- Pureza: 99.19%
- No. CAS: 24533-47-9
- Fòrmula: C18H18O4
- Peso molecular:298.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) L6H21
MoreVer todos los productos específicos de isoformas TNF Receptor
MoreVer todos los productos específicos de isoformas Caspase
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Actividad biológica
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IL-6 8.59 μM (IC50) |
TLR4 |
NF-κB |
NLRP3 inflammasome |
IL-1β |
Caspase 3 |
Bcl-2 |
Bax |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
41.74 μM
Compound: 27
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Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay
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10.1007/s00044-011-9549-9 |
| Peritoneal macrophage | IC50 |
10 μM
Compound: L6H21
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Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA
Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA
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[PMID: 36399795] |
| Peritoneal macrophage | IC50 |
10 μM
Compound: L6H21
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Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA
Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA
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[PMID: 36399795] |
| SGC-7901 | IC50 |
13.08 μM
Compound: 27
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Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay
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10.1007/s00044-011-9549-9 |
L6H21 (10 μM, 2 h) inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells[1].
L6H21 (10 μM, 2 h) attenuates EtOH + LPS-induced ROS formation and TLR4-NF-κB activation, and decreases NLRP3 inflammasome activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells (mouse macrophage cell line)
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Concentration:10 μM
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Incubation Time:2 hours
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Result:Markedly decreased apoptotic cell numbers; completely inhibited EtOH + LPS-induced increase in Bax/Bcl-2; markedly decreased EtOH + LPS-induced elevation in cleaved caspase-3 protein.
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Cell Line:RAW264.7 cells (mouse macrophage cell line)
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Concentration:10 μM
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Incubation Time:2 hours
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Result:Reduced EtOH + LPS-induced TLR4–NF-κB signaling; completely inhibited the increase in TLR4 and NF-κB p65 nuclear level induced by EtOH and LPS. Attenuated EtOH + LPS-induced expression of NLRP3 inflammasome; inhibited the elevated NLRP3 and IL-1β protein expression; decreased the expression of p20, an active form of caspase-1.
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Cell Line:RAW264.7 cells (mouse macrophage cell line)
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Concentration:10 and 20 μM
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Incubation Time:2 hours
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Result:The loss of cell viability by EtOH + LPS was prevented by L6H21 pretreatment. Slightly decreased cell viability a higher dose of 20 μM.
L6H21 (0-40 mg/kg, Orally, daily for 4 weeks) attenuates metabolic disturbance, restores cognition and attenuates brain pathologies dose and time-dependently in HFD-fed rats, and shows neuroprotective effect in a model of prediabetes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6 mice (8-10 weeks old, n = 36, 8 mice in each group, 25-30 g, with EtOH and LPS)[1]
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Dosage:10 mg/kg
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Administration:Oral gavage, daily, before EtOH feeding
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Result:Decreased hepatic triglyceride (TG) concentration, markedly decreased serum alanine transaminase (ALT) and aspartate transaminase (AST) levels; Significantly decreased inflammation in liver tissue induced by EtOH + LPS.
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Animal Model:Male Wistar rats (6-7 weeks old, 250 g, a normal diet (ND) (n=8) or a high-fat diet (HFD) (n=104) for 16 weeks)[2]
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Dosage:0, 10, 20, and 40 mg/kg
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Administration:Orally, daily for 1, 2 or 4 weeks
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Result:Ameliorated brain mitochondrial dysfunction in HFD-fed rats at 2-week administration time point; improved brain mitochondrial function in a dose-dependent manner for 4 weeks. Reduced hippocampal apoptosis in prediabetes for 4 weeks. Attenuated the reduction of dendritic spine volume and density for 4 weeks. Preserved microglial morphology in a dose-dependent manner.
Chemical Information
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No. CAS 24533-47-9
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Appearance Solid
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Peso molecular 298.34
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Fòrmula C18H18O4
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Color White to off-white
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SMILES
O=C(C1=CC=C(OC)C=C1)/C=C/C2=CC=CC(OC)=C2OC
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
A Novel Hybrid Peptide VLP-Aβ Efficiently Regulates Immunity by Stimulating Myeloid Differentiation Protein and Activating the NF-κB Pathway. [Abstract]2025 Jun 18;26(12):5834. PMID: 40565297
Solvente y solubilidad
DMSO : 100 mg/mL (335.19 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, 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.
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.
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 (8.38 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Korean - KR (458 KB)
- Portuguese - PT (458 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kong X, et al. Chalcone Derivative L6H21 Reduces EtOH + LPS-Induced Liver Injury Through Inhibition of NLRP3 Inflammasome Activation. Alcohol Clin Exp Res. 2019 Aug;43(8):1662-1671. [Content Brief]
[2]. Oo TT, et al. L6H21 protects against cognitive impairment and brain pathologies via toll-like receptor 4-myeloid differentiation factor 2 signalling in prediabetic rats. Br J Pharmacol. 2022 Mar;179(6):1220-1236. [Content Brief]
[3]. Yi Wang, et al. MD-2 as the target of a novel small molecule, L6H21, in the attenuation of LPS-induced inflammatory response and sepsis. Br J Pharmacol. 2015 Sep;172(17):4391-405. [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, 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 | 3.3519 mL | 16.7594 mL | 33.5188 mL | 83.7970 mL |
| 5 mM | 0.6704 mL | 3.3519 mL | 6.7038 mL | 16.7594 mL | |
| 10 mM | 0.3352 mL | 1.6759 mL | 3.3519 mL | 8.3797 mL | |
| 15 mM | 0.2235 mL | 1.1173 mL | 2.2346 mL | 5.5865 mL | |
| 20 mM | 0.1676 mL | 0.8380 mL | 1.6759 mL | 4.1899 mL | |
| 25 mM | 0.1341 mL | 0.6704 mL | 1.3408 mL | 3.3519 mL | |
| 30 mM | 0.1117 mL | 0.5586 mL | 1.1173 mL | 2.7932 mL | |
| 40 mM | 0.0838 mL | 0.4190 mL | 0.8380 mL | 2.0949 mL | |
| 50 mM | 0.0670 mL | 0.3352 mL | 0.6704 mL | 1.6759 mL | |
| 60 mM | 0.0559 mL | 0.2793 mL | 0.5586 mL | 1.3966 mL | |
| 80 mM | 0.0419 mL | 0.2095 mL | 0.4190 mL | 1.0475 mL | |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8380 mL |
L6H21 Related Classifications
HY-W082785A Related Classifications
Powered by Bioz
- L6H21
- 24533-47-9
- TNF Receptor
- Interleukin Related
- Toll-like Receptor (TLR)
- NF-κB
- NOD-like Receptor (NLR)
- Apoptosis
- Caspase
- Bcl-2 Family
- Reactive Oxygen Species (ROS)
- Alcoholic Liver Disease
- Lipopolysaccharide
- NLRP3 Inflammasome
- neuroinflammation
- metabolic disturbance
- obesity
- RAW264.7
- MD-2
- myeloid differentiation factor 2
- cognitive deficits
- Inhibitor
- inhibitor
- inhibit