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.
- Formula: C18H10F6O4
- Molecular Weight:404.26
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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STAT1 0.87 μM (IC50) |
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.
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Cell Line:HepG2 cells
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Concentration:0-200 μM (serial 2-fold dilutions starting at 200 μM)
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Incubation Time:24 h
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Result:Showed no cytotoxicity after 24 h of exposure, with no decrease in cell viability even at the highest tested concentration of 200 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 7−8 weeks old, 20-23 g, HF-CDAA diet-induced)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; daily; 4 weeks
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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.
Chemical Information
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Appearance Solid
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Molecular Weight 404.26
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Formula C18H10F6O4
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Color Off-white to light yellow
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SMILES
COC1=C2C(C=C(OC2=CC(O)=C1)C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 83.33 mg/mL (206.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4737 mL | 12.3683 mL | 24.7366 mL | 61.8414 mL |
| 5 mM | 0.4947 mL | 2.4737 mL | 4.9473 mL | 12.3683 mL | |
| 10 mM | 0.2474 mL | 1.2368 mL | 2.4737 mL | 6.1841 mL | |
| 15 mM | 0.1649 mL | 0.8246 mL | 1.6491 mL | 4.1228 mL | |
| 20 mM | 0.1237 mL | 0.6184 mL | 1.2368 mL | 3.0921 mL | |
| 25 mM | 0.0989 mL | 0.4947 mL | 0.9895 mL | 2.4737 mL | |
| 30 mM | 0.0825 mL | 0.4123 mL | 0.8246 mL | 2.0614 mL | |
| 40 mM | 0.0618 mL | 0.3092 mL | 0.6184 mL | 1.5460 mL | |
| 50 mM | 0.0495 mL | 0.2474 mL | 0.4947 mL | 1.2368 mL | |
| 60 mM | 0.0412 mL | 0.2061 mL | 0.4123 mL | 1.0307 mL | |
| 80 mM | 0.0309 mL | 0.1546 mL | 0.3092 mL | 0.7730 mL | |
| 100 mM | 0.0247 mL | 0.1237 mL | 0.2474 mL | 0.6184 mL |
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