PRL-295
PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction. PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice.
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- No. CAS: 2377770-85-7
- Fòrmula: C27H24F3N3O8S2
- Peso molecular:639.62
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Almacenamiento:
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Actividad biológica
Descripciòn
In Vitro
PRL-295 increases the thermostability of Keap1 in Keap1-mCherry-expressing U2OS cells lysates (15 μM, 1 h), HL-60 cells lysates (30 μM, 1 h) and HL-60 cells (10 μM, 3 h)[1].
PRL-295 (50 μM, 1 h) disrupts the Keap1-Nrf2 protein complex in single HeLa cell co-expressing sfGFP-Nrf2 and Keap1-mCherry[1].
PRL-295 (approximately 60 nM-10 μM, 48 h) concentration-dependently induces the Nrf2 target NAD(P)H:quinone oxidoreductase 1 (NQO1) in Hepa1c1c7 and ARPE-19 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PRL-295 (25 mg/kg, p.o., 3 days) protects against Acetaminophen (HY-66005)-induced liver injury in C57/BL6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 wild-type mice[1]
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Dosage:10, 25, 50 mg/kg
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Administration:Oral gavage (p.o.); 4 times, 24 h apart
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Result:Increased hepatic NQO1 mRNA 2.2-fold or 2.8-fold in a dose-dependent manner at 10 mg/kg or 25 mg/kg, respectively.
Increased NQO1 mRNA moderately (1.5-fold) in kidneys at a dose of 25 mg/kg.
Did not significantly increase mRNA levels of NQO1 in the brain, colon, or lung.
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Animal Model:8-week-old male C57/BL6 mice were intraperitoneally Acetaminophen (HY-66005) (300 mg/kg)[1]
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Dosage:25 mg/kg
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Administration:Oral gavage (p.o.); once a day, over a period of 3 days
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Result:Reduced plasma levels of alanine aminotransferase and glutamine aminotransferase.
Chemical Information
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No. CAS 2377770-85-7
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Peso molecular 639.62
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Fòrmula C27H24F3N3O8S2
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SMILES
O=C(CN(S(=O)(C1=CC=C(C=C1)OC)=O)C2=NC=C(N(S(=O)(C3=CC=C(C=C3)OC)=O)CC(F)(F)F)C4=C2C=CC=C4)O
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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
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PRL-295 Related Classifications
HY-171035 Related Classifications
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