1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. ZDZ-553

ZDZ-553 is an orally active STAT1 inhibitor with an IC50 value of 0.87 μM. ZDZ-553 modulates STAT1 signaling to affect downstream lipid metabolism and inflammatory pathways. ZDZ-553 attenuates hepatic steatosis in NASH mouse models. ZDZ-553 reduces inflammatory responses in NASH mouse models. ZDZ-553 can be used for the research of nonalcoholic steatohepatitis.

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

ZDZ-553

ZDZ-553 Chemical Structure

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5 mg Get quote 7 - 9 weeks 6 - 8 weeks 8 - 10 weeks 7 - 9 weeks
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Description

ZDZ-553 is an orally active STAT1 inhibitor with an IC50 value of 0.87 μM. ZDZ-553 modulates STAT1 signaling to affect downstream lipid metabolism and inflammatory pathways. ZDZ-553 attenuates hepatic steatosis in NASH mouse models. ZDZ-553 reduces inflammatory responses in NASH mouse models. ZDZ-553 can be used for the research of nonalcoholic steatohepatitis[1].

IC50 & Target[1]

STAT1

0.87 μM (IC50)

In Vitro

ZDZ-553 (24 h) potently inhibits STAT1 activity in stable 293T-STAT1/GAS-Luc cells with an IC50 of 0.87 μM and shows no cytotoxicity at concentrations up to 200 μM[1].
ZDZ-553 (0.052 μM; 0, 30, 60, 120 min) has excellent metabolic stability in human, mouse, and rat liver microsomes, with a T1/2 >120 min across all species[1].
ZDZ-553 (0-200 μM; 24 h) exhibits no cytotoxicity in HepG2 cells at concentrations up to 200 μM[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 cells
Concentration: 0-200 μM (serial 2-fold dilutions starting at 200 μM)
Incubation Time: 24 h
Result: Showed no cytotoxicity after 24 h of exposure, with no decrease in cell viability even at the highest tested concentration of 200 μM.
Parmacokinetics
Species Dose Route AUC0-inf Cmax T1/2 MRT0-inf Tmax F
Rat[1] 30 mg/kg i.v. 69,512 ng·h/mL 2467 ng/mL 16.63 h 24.3 h / /
Rat[1] 30 mg/kg p.o. 12,599 ng·h/mL 819 ng/mL 12.18 h 18.8 h 1.13 h 18.1 %
In Vivo

ZDZ-553 (30-60 mg/kg; p.o.; daily; 4 weeks) administered orally at 30 and 60 mg/kg for 4 weeks dose-dependently ameliorates hepatic steatosis, liver damage, and inflammation in HF-CDAA-induced NASH mice, with the 60 mg/kg dose showing greater efficacy than the 30 mg/kg dose and the positive control Dios[1].

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

Animal Model: C57BL/6J (male, 7−8 weeks old, 20-23 g, HF-CDAA diet-induced)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; 4 weeks
Result: Reduced hepatic triglyceride (TG) and total cholesterol (TC) levels, reduced serum ALT and AST levels; reduced mRNA expression of hepatic acetyl-CoA carboxylase (ACC), fatty acid synthase (FASN), FATP-1, IL-6, IL-1β, TNF-α, and CXCL10; decreased NAFLD Activity Score (NAS) compared to vehicle controls; reduced hepatocellular ballooning (H&E staining) and reduced size/quantity of lipid droplets (Oil Red O staining) at 30 mg/kg.
Produced greater dose-dependent reductions in hepatic TG, TC, serum AST, and mRNA expression of ACC, FASN, FATP-1, IL-6, IL-1β, TNF-α, and CXCL10 compared to the 30 mg/kg dose; resulted in a larger decrease in NAS compared to the 30 mg/kg dose; showed more pronounced improvements in hepatocellular ballooning and lipid droplet accumulation (histological staining) compared to the 30 mg/kg dose at 60 mg/kg.
Showed more significant reductions in hepatic TG, TC, serum AST, and inflammatory cytokine mRNA expression than the positive control Dios at 60 mg/kg at both doses.
Molecular Weight

404.26

Formula

C18H10F6O4

SMILES

COC1=C2C(C=C(OC2=CC(O)=C1)C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O

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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Help & FAQs
  • 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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ZDZ-553
Cat. No.:
HY-181792
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