1. Metabolic Enzyme/Protease NF-κB Apoptosis Immunology/Inflammation Membrane Transporter/Ion Channel
  2. Xanthine Oxidase NF-κB TNF Receptor Interleukin Related URAT1 GLUT
  3. Xanthine oxidase-IN-21

Xanthine oxidase-IN-21, a Genipin (HY-17389) derivative, is an orally active mixed competitive xanthine oxidase (XOD) inhibitor with an IC50 of 0.68 μM. Xanthine oxidase-IN-21 reduces renal fibrosis by decreasing α-SMA expression and suppresses pro-inflammatory cytokines IL-1β, IL-6, and TNF-α through NF-κB pathway regulation. Xanthine oxidase-IN-21 also inhibits URAT1 and GLUT9 expression, promoting uric acid excretion and lowering serum uric acid levels. Xanthine oxidase-IN-21 shows significantly hepatorenal protection activity. Xanthine oxidase-IN-21 can be used for the research of hyperuricemia.

For research use only. We do not sell to patients.

Xanthine oxidase-IN-21

Xanthine oxidase-IN-21 Chemical Structure

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Description

Xanthine oxidase-IN-21, a Genipin (HY-17389) derivative, is an orally active mixed competitive xanthine oxidase (XOD) inhibitor with an IC50 of 0.68 μM. Xanthine oxidase-IN-21 reduces renal fibrosis by decreasing α-SMA expression and suppresses pro-inflammatory cytokines IL-1β, IL-6, and TNF-α through NF-κB pathway regulation. Xanthine oxidase-IN-21 also inhibits URAT1 and GLUT9 expression, promoting uric acid excretion and lowering serum uric acid levels. Xanthine oxidase-IN-21 shows significantly hepatorenal protection activity. Xanthine oxidase-IN-21 can be used for the research of hyperuricemia[1].

IC50 & Target[1]

Xanthine oxidase

0.68 μM (IC50)

NF-κB

 

IL-1β

 

IL-6

 

In Vitro

Xanthine oxidase-IN-21 (compound 5b) (0.1, 1, 10, 100, and 200 μM; 24 h) is non-cytotoxicity to HK-2 cells[1].

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

In Vivo

Xanthine oxidase-IN-21 (compound 5b) (10-30 mg/kg, oral, daily, for 2 weeks) reduces uric acid levels, protects liver and kidney function, and ameliorates inflammation and fibrosis in Hyperuricemic mice[1].

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

Animal Model: A hyperuricemia model was established in KM (male, 20 g) by injection of Adenine (HY-B0152) and Potassium oxonate (PO) (HY-17511)[1]
Dosage: 10 mg/kg, 20 mg/kg, 30 mg/kg
Administration: Oral; daily; for 2 weeks
Result: Significantly reduced serum uric acid (UA) levels, creatinine (Cr), and blood urea nitrogen (BUN) in hyperuricemic mice.
Also decreased the levels of AST and ALT, indicating protection of liver and kidney function.
Ameliorated kidney and liver damage, reduced inflammatory cytokine levels (IL-1β, IL-6, TNF-α), and decreased the expression of pro-inflammatory markers (p-ERK, p-p38, p65 NF-κB).
Reduced the expression of uric acid transporters (URAT1, GLUT9) and inhibited XOD activity, which is a key target in hyperuricemia.
Molecular Weight

338.40

Formula

C20H22N2O3

SMILES

O=C(OC)C1=CCC(OC)C2C1CC=C2CNC3=CC=C(C#N)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Xanthine oxidase-IN-21
Cat. No.:
HY-180271
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