UCM-17017
UCM-17017 is a tetrasubstituted cyclohexene inhibitor that inhibits the activity of senescent cell SA-β-gal with an IC50 of 0.4 μM. UCM-17017 selectively reduces the viability of senescent cancer cells, and this effect is stronger than its impact on proliferating cells. UCM-17017 binds to human serum albumin with a KD of 230 μM. UCM-17017 reduces collagen deposition and decreases the expression of the inflammatory marker Ccl2 in a mouse model of pulmonary fibrosis. UCM-17017 can be used in studies related to senescence and pulmonary fibrosis.
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- Fòrmula: C18H25FN2
- Peso molecular:288.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
SA-β-gal 0.4 μM (IC50) |
In Vitro
UCM-17017 (200 μM; 5 h) exhibits a permeability value of 8.4 × 10-6 cm/s in cell-free PAMPA assays[1].
UCM-17017 exhibits a half-life of over 48 h in human and mouse serum, demonstrating high serum stability[1].
UCM-17017 exhibits favorable metabolic stability in human and mouse liver microsomes, with half-lives of 5.0 h and 2.2 h, respectively[1].
UCM-17017 binds to human serum albumin with an occupancy rate of 72% and a KD of 230 μM[1].
UCM-17017 (100 μM; 30 min) does not inhibit hERG potassium channels, indicating a low risk of cardiotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:bleomycin-induced senescent human lung adenocarcinoma (A549) cells, proliferative A549 cells
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Concentration:1 μM, 10 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Selectively reduced viability of senescent A549 cells compared to proliferative A549 cells.
Showed the greatest selectivity after 48-72 h post-treatment at both 1 μM and 10 μM.
Resulted in a viability ratio of proliferative to senescent A549 cells of approximately 1.3-fold.
Parmacokinetics
| Species | Dose | Route | C0 | Vd | T1/2 | AUC | CL |
|---|---|---|---|---|---|---|---|
| Mice[1] | 40 mg/kg | i.p. | 111 μg/L | 365 L/kg | 1.87 h | 0.30 mg·h/L | 137 |
In Vivo
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, 10 weeks old, bleomycin-induced pulmonary fibrosis)[1]
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Dosage:40 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Significantly reduced collagen deposition in lung tissue to levels similar to the reference senolytic ABT-263.
Downregulated mRNA expression levels of the inflammation marker *Ccl2*.
Did not significantly reduce SA-β-gal activity.
Did not affect bleomycin-induced weight loss.
Did not induce structural damage, apoptosis, or toxicity in liver and kidney tissues.
- Fibrosis/Collagen Morphometry
- Collagen: Sirius Red Staining
- RNA extraction experimental
- Ki-67 Immunostaining Proliferation Assay
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Senescence-associated β-galactosidase staining
- Cell Viability Determination by MTT Colorimetric Assay
- How to Choose the Right Model Animal
Chemical Information
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Peso molecular 288.40
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Fòrmula C18H25FN2
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SMILES
N[C@@H]1[C@@H](C2=CC=C(F)C=C2)[C@H](C)C=C(CNCC3CC3)C1
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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)
UCM-17017 Related Classifications
HY-187365 Related Classifications
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