CBS-3408
CBS-3408 is an orally active p38α MAPK inhibitor. CBS-3408 inhibits the release of TNFα and IL-1β. CBS-3408 reduces the disease severity of arthritis in mice. CBS-3408 inhibits TNFα release in a rat endotoxemia model. CBS-3408 can be used in studies related to endotoxemia and arthritis.
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- No. CAS: 452056-93-8
- Fòrmula: C18H17FN4OS
- Peso molecular:356.42
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Almacenamiento:
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Ver todos los productos específicos de isoformas TNF Receptor
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
28.6 μM
Compound: 3; CBS-3408
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Inhibition of human ERG expressed in HEK293 cells by patch clamp method
Inhibition of human ERG expressed in HEK293 cells by patch clamp method
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[PMID: 28613871] |
CBS-3408 (Compound 3) inhibits LPS (HY-D1056)-induced IL-1β and TNFα release in human whole blood[1].
CBS-3408 (10 μM) inhibits JNK3 and p38β kinases by over 70%[1].
CBS-3408 (10 μM) inhibits CYP2C9 (46%) and CYP2D6 (45%), shows weak inhibitory activity against CYP1A2 (18%), and exhibits no relevant activity against CYP2C19 or CYP3A4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | AUC0-t | T1/2 |
|---|---|---|---|---|---|---|
| Rat[1] | 30 mg/kg | p.o. | 1.0 h | 738 ng/mL | 4928 ng·h/mL | 3.0 h |
CBS-3408 (50 mg/kg; p.o.; twice daily) significantly reduces the disease severity of collagen (HY-NP003)-induced arthritis in male DBA/1 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Achieved 97% inhibition of plasma TNFα concentrations compared to control animals.
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Animal Model:DBA/1 (male)[1]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily
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Result:Substantially reduced arthritic disease severity, with a notably lower arthritic score compared to vehicle control animals over the course of the study.
Showed no treatment-related toxicity aside from body weight loss identical to controls.
Chemical Information
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No. CAS 452056-93-8
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Peso molecular 356.42
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Fòrmula C18H17FN4OS
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SMILES
O=C(C)NC1=NC=CC(C2=C(C3=CC=C(C=C3)F)N=C(N2C)SC)=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)
CBS-3408 Related Classifications
HY-182579 Related Classifications
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