1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Ferroptosis Reactive Oxygen Species (ROS)
  3. 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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YL3147

YL3147 Chemical Structure

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Description

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[1].

In Vitro

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.

Cell Cytotoxicity Assay[1]

Cell Line: Multiple normal human cell lines (BEAS-2B, HUVEC, AC16, GES-1, HK-2, HaCaT, ARPE-19, hTERT-HPNE)
Concentration: /
Incubation Time: 72 h
Result: Exhibited minimal cytotoxicity, with CC50 values >10 μM across all tested normal cell lines.
Parmacokinetics
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 /
In Vivo

YL3147 (10-30 mg/kg; i.p.; single dose/3 weeks) exerts cardioprotective effects in Doxorubicin (HY-15142A)-induced acute and chronic cardiomyopathy mouse models[1].
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.

Animal Model: C57BL/6 (8-week-old male; acute Doxorubicin-induced cardiomyopathy model)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; single dose 2 hours prior to doxorubicin
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.
Animal Model: C57BL/6 (8-week-old male; chronic doxorubicin-induced cardiomyopathy model)[1]
Dosage: 30 mg/kg
Administration: i.p.; daily; 3 consecutive weeks, starting 3 days before first doxorubicin dose
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.
Molecular Weight

402.51

Formula

C25H27FN4

SMILES

FC1=CC(C2=CC3=C(CNC4=CC=CC=C4N3)C(N5CC(N(CC5)C)C)=C2)=CC=C1

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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Product Name:
YL3147
Cat. No.:
HY-181548
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