HGR4113
HGR4113 is an orally active anti-inflammatory/antioxidant agent with improved glucose metabolism. HGR4113 inhibits STAT3 phosphorylation, suppresses Th17 differentiation and IL-17 production, reduces oxidative phosphorylation activity, and promotes the differentiation of regulatory T cells among splenic CD4+ T cells. HGR4113 inhibits LPS (HY-D1056)-induced JNK phosphorylation, production of NO, PGE2 and pro-inflammatory cytokines, expression of iNOS and COX-2, as well as nuclear translocation of NF-κB in macrophages, while induces HO-1 expression by activating nuclear translocation of Nrf2. HGR4113 can be used in the research of inflammatory diseases such as type 2 diabetes and Sjögren's syndrome.
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- No. CAS: 2170918-46-2
- Fòrmula: C23H28O4
- Peso molecular:368.47
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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STAT3 |
iNOS |
COX-2 |
IL-17 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
11.32 μM
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Inhibition of LPS-induced nitric oxide production in RAW264.7 macrophages assessed via Griess reaction after 3 h pre-treatment with reagent followed by 24 h LPS stimulation.
Inhibition of LPS-induced nitric oxide production in RAW264.7 macrophages assessed via Griess reaction after 3 h pre-treatment with reagent followed by 24 h LPS stimulation.
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36903379 |
| RAW264.7 | IC50 |
1.64 μM
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Inhibition of LPS-induced prostaglandin E2 production in RAW264.7 macrophages assessed via ELISA after 3 h pre-treatment with reagent followed by 24 h LPS stimulation.
Inhibition of LPS-induced prostaglandin E2 production in RAW264.7 macrophages assessed via ELISA after 3 h pre-treatment with reagent followed by 24 h LPS stimulation.
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36903379 |
HGR4113 (1-10 μM; 74 h) reduces the viability of stimulated splenocytes in a dose-dependent manner, and inhibits the production of pro-inflammatory cytokines IFNγ, IL-17, TNF-α and IL-6 in splenocytes from C57BL/6 and NOD/ShiLtJ mice stimulated with anti-CD3/anti-CD28 antibodies or LPS[1].
HGR4113 (1-10 μM; 74 h) dose-dependently inhibits Th17 differentiation and pro-inflammatory cytokine production, promotes Treg differentiation, suppresses STAT3 phosphorylation, and reduces OXPHOS activity in purified splenic CD4+ T cells from C57BL/6 mice[1].
HGR4113 (1-10 μM; 98 h) dose-dependently shifts the polarization of B cells from proinflammatory IL-17-producing cells to regulatory IL-10-producing cells, reduces immunoglobulin production, and modulates the mRNA expression of B cell activation- and fibrosis-related genes in purified splenic CD19+ B cells from C57BL/6 mice[1].
HGR4113 (27 h) inhibits LPS-induced NO production in RAW264.7 macrophages in a dose-dependent manner, with an IC50 of 11.32 μM[2].
HGR4113 (5-20 μM; 27 h) reduces LPS-induced iNOS and COX-2 protein expression in RAW264.7 macrophages in a dose-dependent manner[2].
HGR4113 (5-20 μM; 4 h) inhibits LPS-induced NF-κB activation in RAW264.7 macrophages in a dose-dependent manner by reducing the phosphorylation level of IκB-α, NF-κB nuclear translocation, and NF-κB DNA-binding activity[2].
HGR4113 (5-20 μM; 3.5 h) dose-dependently inhibits LPS-induced phosphorylation of JNK in RAW264.7 macrophages without affecting the phosphorylation of ERK or p38[2].
HGR4113 (5-20 μM; 12 h) dose-dependently induces the expression of HO-1 protein in RAW264.7 macrophages[2].
HGR4113 (20 μM; 0.5-1.5 h) induces nuclear translocation of Nrf2 in RAW264.7 macrophages, increases nuclear Nrf2 levels and decreases cytoplasmic Nrf2 levels over time[2].
HGR4113 (20 μM; 15 h) induces the expression of HO-1 protein in RAW264.7 macrophages via the ERK MAPK pathway, while the p38 and JNK MAPK pathways exert negative regulatory effects on this induction process[2].
HGR4113 (5-20 μM; 27 h) dose-dependently inhibits LPS-induced PGE2 production in RAW264.7 macrophages, with an IC50 value of 1.64 μM[2].
HGR4113 (5-20 μM; 9 h) dose-dependently inhibits LPS-induced expression of IL-1β, IL-6 and TNF-α mRNA in RAW264.7 macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 macrophages
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Concentration:5, 10 20 μM
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Incubation Time:3 h pre-treatment, followed by 24 h LPS stimulation
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Result:Dose-dependently reduced LPS-induced PGE2 production.
Inhibited PGE2 production with an IC50 of 1.64 μM.
Showed inhibitory effects comparable to the positive control butein at 20 μM.
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Cell Line:RAW264.7 macrophages
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Concentration:5, 10 and 20 μM
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Incubation Time:3 h pre-treatment, followed by 24 h LPS stimulation
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Result:Dose-dependently reduced LPS-induced iNOS and COX-2 protein expression.
Reduced iNOS protein levels to 0.64 relative to actin at 20 μM.
Reduced COX-2 protein levels to 0.65 relative to actin at 20 μM.
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Cell Line:RAW264.7 macrophages
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Concentration:5, 10 and 20 μM
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Incubation Time:3 h pre-treatment, followed by 6 h LPS stimulation
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Result:Dose-dependently reduced LPS-induced IL-1β, IL-6, and TNF-α mRNA expression.
Showed inhibitory effects comparable to the positive control butein at 20 μM.
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Cell Line:RAW264.7 macrophages
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Concentration:5, 10 and 20 μM
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Incubation Time:3 h pre-treatment, followed by 30 min LPS stimulation
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Result:Dose-dependently reduced LPS-induced JNK phosphorylation.
Showed no effect on ERK or p38 phosphorylation.
Reduced p-JNK levels to 0.54 relative to actin at 20 μM.
Left total unphosphorylated MAPK levels unaffected.
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Cell Line:RAW264.7 macrophages
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Concentration:5-20 μM
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Incubation Time:12 h
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Result:Dose-dependently increased HO-1 protein expression.
Increased HO-1 levels to 1.84 relative to actin at 20 μM.
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Cell Line:RAW264.7 macrophages
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Concentration:20 μM
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Incubation Time:0.5, 1, 1.5 h
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Result:Increased nuclear Nrf2 expression over the 1.5 h treatment period.
Decreased cytosolic Nrf2 expression over the 1.5 h treatment period.
Increased nuclear Nrf2 levels to 1.92 relative to PCNA at 1.5 h.
Decreased cytosolic Nrf2 levels to 0.60 relative to actin at 1.5 h.
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Cell Line:RAW264.7 macrophages
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Concentration:20 μM
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Incubation Time:12 h after 3 h pre-incubation with MAPK inhibitors
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Result:Reduced HO-1 expression to 0.70 relative to actin when pre-treated with ERK inhibitor PD98059 (HY-12028).
Increased HO-1 expression to 1.13 relative to actin when pre-treated with p38 inhibitor SB203580 (HY-10256).
Increased HO-1 expression to 1.55 relative to actin when pre-treated with JNK inhibitor SP600125 (HY-12041).
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[1] | 160 mg/kg | p.o. | 4.90 μg/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/ShiLtJ (8-week-old female)[1]
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Dosage:100 mg/kg
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Administration:p.o.; once daily; 12 weeks
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Result:Maintained higher salivary flow rates than vehicle-treated mice through week 20.
Reduced serum total IgG levels.
Decreased salivary gland infiltration of CD4+ cells, CD19+ cells, IL-6+ cells, and IL-17+ cells.
Reduced splenic frequencies of Th17 cells, CD4+ICOS+IFNγ+Bcl6+ follicular helper T cells, CD4+ICOS+IL-17+Bcl6+ follicular helper T cells, germinal-centre B cells, and plasma cells.
Reduced salivary gland fibrosis area, collagen I-positive area, fibronectin-positive area, and TGF-β-positive area; increased aquaporin-5-positive area in salivary glands.
Enhanced formation of 3D salivary epithelial structures, with increased fluorescence intensity of E-cadherin, aquaporin-5, α-SMA, and cytokeratin-14 in these structures.
Chemical Information
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No. CAS 2170918-46-2
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Peso molecular 368.47
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Fòrmula C23H28O4
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SMILES
CCCOC1=CC=C(C(O)=C1)[C@@H]2COC3=C4CCC(C)(OC4=CC=C3C2)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HGR4113 Related Classifications
HY-187690 Related Classifications
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