Cat. No.: HY-187690

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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CAS No.: 2170918-46-2
화학식: C₂₃H₂₈O₄
분자량:368.47

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

HGR4113 Chemical Structure

CAS No.: 2170918-46-2

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]^[2]

STAT3

iNOS

COX-2

IL-17

All STAT Isoforms :

All JNK Isoforms :

All NO Synthase Isoforms :

All COX Isoforms :

All NF-κB Isoforms :

All Interleukin Related Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
RAW264.7	IC50	11.32 μM	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.	36903379
RAW264.7	IC50	1.64 μM	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.	36903379

In Vitro

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.

ELISA Assay^[2]

Cell Line:

RAW264.7 macrophages
Concentration:

5, 10 20 μM
Incubation Time:

3 h pre-treatment, followed by 24 h LPS stimulation
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.

Western Blot Analysis^[2]

Cell Line:

RAW264.7 macrophages
Concentration:

5, 10 and 20 μM
Incubation Time:

3 h pre-treatment, followed by 24 h LPS stimulation
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.

Real Time qPCR^[2]

Cell Line:

RAW264.7 macrophages
Concentration:

5, 10 and 20 μM
Incubation Time:

3 h pre-treatment, followed by 6 h LPS stimulation
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.

Western Blot Analysis^[2]

Cell Line:

RAW264.7 macrophages
Concentration:

5, 10 and 20 μM
Incubation Time:

3 h pre-treatment, followed by 30 min LPS stimulation
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.

Western Blot Analysis^[2]

Cell Line:

RAW264.7 macrophages
Concentration:

5-20 μM
Incubation Time:

12 h
Result:

Dose-dependently increased HO-1 protein expression.
Increased HO-1 levels to 1.84 relative to actin at 20 μM.

Western Blot Analysis^[2]

Cell Line:

RAW264.7 macrophages
Concentration:

20 μM
Incubation Time:

0.5, 1, 1.5 h
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.

Western Blot Analysis^[2]

Cell Line:

RAW264.7 macrophages
Concentration:

20 μM
Incubation Time:

12 h after 3 h pre-incubation with MAPK inhibitors
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).

Parmacokinetics

Species	Dose	Route	C_max
Mice^[1]	160 mg/kg	p.o.	4.90 μg/mL

In Vivo

HGR4113 (100 mg/kg; p.o.; once daily; 12 weeks) alleviates SS-like symptoms in 8-week-old female NOD/ShiLtJ mice by reducing immune cell infiltration, inflammation, and fibrosis in salivary glands, restoring salivary function, and promoting 3D salivary epithelial structure maturation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD/ShiLtJ (8-week-old female)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once daily; 12 weeks
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

CAS No. 2170918-46-2
분자량 368.47
화학식 C₂₃H₂₈O₄
SMILES

CCCOC1=CC=C(C(O)=C1)[C@@H]2COC3=C4CCC(C)(OC4=CC=C3C2)C
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Park JS, et al. Therapeutic effects of a synthetic glabridin derivative on metabolic immuno-regulation and salivary gland functional restoration in experimental Sjögren's syndrome. Experimental & molecular medicine. 2026 Jul;58(7):2356-2367.

[2]. Shin J, et al. Synthetic Glabridin Derivatives Inhibit LPS-Induced Inflammation via MAPKs and NF-κB Pathways in RAW264.7 Macrophages. Molecules (Basel, Switzerland). 2023 Feb 24;28(5):2135.

Calculators

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Molecular Weight Molecular Weight

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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HGR4113

All STAT Isoforms

All JNK Isoforms

All NO Synthase Isoforms

All COX Isoforms

All NF-κB Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

HGR4113 Related Classifications

HY-187690 Related Classifications

Bioz