YL3147
YL3147 is a ferroptosis inhibitor. YL3147 also acts as a radical-trapping antioxidant that directly prevents the spread of lipid peroxidation and blocks ferroptosis. YL3147 exerts significant cardioprotective effects in mouse cardiomyopathy models. YL3147 can be used in studies related to cardiomyopathy.
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- CAS No.: 3123207-48-4
- Formule: C25H27FN4
- Masse moléculaire:402.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
YL3147 (48 h) protects ES-2, AC16, HT1080, and PANC-1 cells from Erastin (HY-15763)-induced ferroptosis with EC50 values of 0.8, 0.8, 0.43, and 0.92 nM, respectively[1].
YL3147 (0.01-1 μM; 10-12 h) effectively alleviates Erastin (HY-15763)-induced lipid peroxidation in ES-2 and AC16 cells, as well as ROS production in ES-2 cells[1].
YL3147 (72 h) exhibits low cytotoxicity against various human normal cell lines, with a CC50 value greater than 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Multiple normal human cell lines (BEAS-2B, HUVEC, AC16, GES-1, HK-2, HaCaT, ARPE-19, hTERT-HPNE)
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Concentration:/
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Incubation Time:72 h
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Result:Exhibited minimal cytotoxicity, with CC50 values >10 μM across all tested normal cell lines.
| Species | Dose | Route | AUC0-t | AUC0-∞ | Cmax | CL | Vz/F | T1/2 | Tmax | MRT0-t | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 3794.61 μg/L·h | 3800.28 μg/L·h | 584.18 μg/L | 2.63 L/h/kg | 9.28 L/kg | 2.44 h | 1.00 h | 4.65 h | 53.04 % |
| Mice[1] | 10 mg/kg | i.v. | 7022.24 μg/L·h | 7078.71 μg/L·h | 2537.57 μg/L | 1.49 L/h/kg | 6.94 L/kg | 3.35 h | 0.08 h | 4.31 h | / |
| Mice[1] | 10 mg/kg | i.p. | 5033.34 μg/L·h | 5050.96 μg/L·h | 549.69 μg/L | 1.98 L/h/kg | 8.31 L/kg | 2.91 h | 0.25 h | 6.08 h | / |
YL3147 (200 mg/kg; p.o.; single dose) is well tolerated in BALB/c mice, with no acute toxicity or organ injury detected[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (8-week-old male; acute Doxorubicin-induced cardiomyopathy model)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; single dose 2 hours prior to doxorubicin
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Result:Significantly improved cardiac function, including increased ejection fraction, cardiac output, and stroke volume, relative to vehicle-treated mice.
Prolonged survival and reduced mortality relative to vehicle-treated mice.
Markedly reduced doxorubicin-induced elevation in serum lactate dehydrogenase (LDH) and creatine kinase-MB (CK-MB) levels.
Suppressed increases in myocardial malondialdehyde (MDA) content and mRNA levels of cardiac stress gene Myh7 and ferroptosis-related marker Ptgs2.
Preserved cardiomyocyte structure, attenuated cardiac fibrosis, and reduced 4-hydroxynonenal (4-HNE) immunopositivity in heart tissue.
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Animal Model:C57BL/6 (8-week-old male; chronic doxorubicin-induced cardiomyopathy model)[1]
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Dosage:30 mg/kg
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Administration:i.p.; daily; 3 consecutive weeks, starting 3 days before first doxorubicin dose
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Result:Reduced mortality and attenuated weight loss relative to vehicle-treated mice.
Attenuated doxorubicin-induced ventricular remodeling, with improved ejection fraction, fractional shortening, cardiac output, and stroke volume relative to vehicle-treated mice.
Reduced serum levels of cardiac injury markers LDH and CK-MB relative to vehicle-treated mice.
Decreased myocardial MDA content and attenuated upregulation of Myh7 and Ptgs2 mRNA expression relative to vehicle-treated mice.
Preserved cardiomyocyte architecture, reduced cardiac fibrosis, and lowered tissue lipid peroxidation (4-HNE immunopositivity) relative to vehicle-treated mice.
Caused no significant changes in body weight, cardiac function parameters, serum organ damage markers (ALT, AST, creatinine), or histopathological architecture of major organs when used as monotherapy.
Chemical Information
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CAS No. 3123207-48-4
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Masse moléculaire 402.51
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Formule C25H27FN4
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SMILES
FC1=CC(C2=CC3=C(CNC4=CC=CC=C4N3)C(N5CC(N(CC5)C)C)=C2)=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YL3147 Related Classifications
HY-181548 Related Classifications
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