PI3K-001
PI3K-001 is a cathepsin B-responsive prodrug and antifibrotic agent. PI3K-001 undergoes cathepsin B-mediated cleavage of the Val-Ala linker in fibrotic lung lesions to release an active PI3K inhibitor payload, while it remains stable in healthy tissues. PI3K-001 improves collagen deposition, tissue collapse and alveolar injury in fibrotic lung tissues. PI3K-001 is applicable for the research of pulmonary fibrosis.
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- Fòrmula: C82H111F2N11O22S2
- Peso molecular:1704.95
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
PI3K-001 (50 μM; 30 min at 37 °C) binds to albumin with a rate exceeding 97% in both human and mouse plasma[1].
PI3K-001 (50 μM; 1-7 days at 37 °C) exhibits high plasma stability, with less than 1% release of its active payload P001 over 7 days of incubation at 37 °C in both human and mouse plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PI3K-001 (25 mg/kg; i.v.; once every 7 days; 2 total doses) exhibits superior antifibrotic efficacy in a bleomycin-induced pulmonary fibrosis mouse model, including significantly improved survival, reduced body weight loss, and reduced lung fibrosis markers compared to the parent drug P001[1].
PI3K-001 (3 mg/kg; i.v.; single dose) demonstrates improved pharmacokinetic properties in healthy SD rats, with 10-fold higher Cmax and 7-fold higher AUC than the parent drug P001, indicating enhanced systemic exposure and prolonged circulation[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 (male, 20-22 g, bleomycin-induced pulmonary fibrosis)[1]
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Dosage:9.5 mg/kg
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Administration:i.v.; single dose
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Result:Delivered P001 to lung tissue at a concentration significantly higher than the parent P001 group at 6 h post-administration.
Maintained detectable P001 in lung tissue at up to ~50 ng/g at 18 h post-administration, while P001 was nearly undetectable in lung tissue.
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Animal Model:C57BL/6 (male, bleomycin-induced pulmonary fibrosis)[1]
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Dosage:25 mg/kg
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Administration:i.v.; once every 7 days; 2 total doses
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Result:Significantly improved mouse survival compared to the P001 group.
Reduced body weight loss relative to the P001 group.
Produced statistically significant reductions in bleomycin-induced increases in lung weight and lung index, with greater improvement than P001 and the positive control nintedanib.
Significantly reduced lung collagen deposition and preserved alveolar structure, with lung tissue morphology closer to normal than the P001 group, as shown by Masson and H&E staining.
Chemical Information
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Peso molecular 1704.95
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Fòrmula C82H111F2N11O22S2
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SMILES
COC1=C(C=C(C=N1)C2=CC3=C(N=CC=C3C4=CN=C(C=C4)COCN(C(OCC5=CC=C(C=C5)NC([C@@H](NC([C@H](C(C)C)NC(COCCOCCNC(COCCOCCNC(CC[C@@H](NC(CCCCCCCCCCCCCCCCC(O)=O)=O)C(O)=O)=O)=O)=O)=O)C)=O)=O)CCS(C)(=O)=O)C=C2)NS(=O)(C6=CC=C(C=C6F)F)=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)
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