L6H21

SKU: orb2900591

Description

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 andIL-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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Key Properties

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CAS Number	24533-47-9
MW	298.33
Purity	>98% (HPLC)
Formula	C₁₈H₁₈O₄
SMILES	O(C)C1=C(/C=C/C(=O)C2=CC=C(OC)C=C2)C=CC=C1OC
Target	NF-κB
Solubility	In Vitro: DMSO : 100 mg/mL (335.20 mM; Ultrasonic )

Bioactivity

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In Vivo

L6H21 (10 mg/kg, Oral gavage, daily) effectively inhibits EtOH + LPS-induced hepatic fat accumulation, hepatic steatosis and liver injury. 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. Animal model: Male C57BL6 mice (8-10 weeks old, n = 36, 8 mice in each group, 25-30 g, with EtOH and LPS). Dosage: 10 mg/kg. Administration: Oral gavage, daily, before EtOH feeding. 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. 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). Dosage: 0, 10, 20, and 40 mg/kg. Administration: Orally, daily for 1, 2 or 4 weeks. 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.

In Vitro

L6H21 (10 μM, 2 h) inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells. L6H21 (10 μM, 2 h) attenuates EtOH + LPS-induced ROS formation and TLR4-NF-κB activation, and decreases NLRP3 inflammasome activation. Apoptosis Analysis Cell line: RAW264.7 cells (mouse macrophage cell line) Concentration: 10 μM. Incubation time: 2 hours. 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. Western blot analysis. Cell line: RAW264.7 cells (mouse macrophage cell line) Concentration: 10 μM. Incubation time: 2 hours. 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.Cell Viability Assay Cell line: RAW264.7 cells (mouse macrophage cell line) Concentration: 10 and 20 μM. Incubation time: 2 hours. Result: The loss of cell viability by EtOH + LPS was prevented by L6H21 pretreatment. Slightly decreased cell viability a higher dose of 20 μM.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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L6H21 (orb2900591)

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Purity:	99.26% (May vary between batches)
CAS Number:	24533-47-9
MW:	298.33
Formula:	C₁₈H₁₈O₄

L6H21

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

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