CLP-d2
CLP-d2 is a multi-target anti-inflammatory agent, osteoclastogenesis inhibitor and immunomodulator with superior pharmacokinetic properties to Daptomycin (HY-B0108) and good safety profiles. CLP-d2 inhibits the NF-κB and MAPK signaling pathways by reducing the expression levels of c-Fos and NFATc1, and decreasing the phosphorylation levels of IκBα, p65, ERK and JNK, thereby reducing the secretion of pro-inflammatory cytokines such as IL-6, TNF-α and IL-1β to exert anti-inflammatory activity. CLP-d2 inhibits intra-articular osteoclastogenesis in mice, alleviates bone erosion and joint swelling, reduces synovial hyperplasia and inflammatory cell infiltration, and decreases serum rheumatoid factor (RF) levels. CLP-d2 is applicable to related research on rheumatoid arthritis.
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- Fòrmula: C78H104N18O27
- Peso molecular:1725.76
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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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p65 |
IL-6 |
IL-1β |
I-kappaBalpha |
CLP-d2 (10 μg/mL; 24 h) potently uppresses the secretion of pro-inflammatory cytokines and their transcription levels in RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells
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Concentration:10 μg/mL
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Incubation Time:24 h
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Result:Inhibits secretion and gene transcription of IL-6, TNF-α, and IL-1β in LPS-stimulated RAW264.7 cells, with the greatest inhibition of IL-6 (93.7% reduction in gene level)
CLP-d2 (10 mg/kg; i.v.; single dose) exhibits favorable pharmacokinetic parameters in Balb/c mice, including a larger AUC0-t and longer T1/2 compared to daptomycin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/1J male mice (6−7 weeks)[1]
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Dosage:10 mg/kg
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Administration:i.v.; every 2 days; 40 days
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Result:Increased body weight by 12% compared to the CIA group; reduced arthritis score by 45.9% compared to the CIA group; reduced serum RF levels by 46.0%, serum IL-6 levels by 54.2%, serum TNF-α levels by 25.9%, and serum IL-1β levels by 42.6% compared to the CIA group; reduced joint histopathological scores by 70.4% compared to the CIA group; reduced IL-6 IHC scores by 46.4%, IL-1β IHC scores by 59.2%, and TNF-α IHC scores by 49.3% compared to the CIA group; reduced p-IκBα IHC scores by 59.3%, p-p65 IHC scores by 58.6%, p-ERK IHC scores by 60.9%, p-JNK IHC scores by 58.6%, c-Fos IHC scores by 59.1%, and NFATc1 IHC scores by 66.6% compared to the CIA group; reduced bone erosion and paw swelling; inhibited p65 nuclear translocation and osteoclast generation in joints.
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Animal Model:Balb/c mice[1]
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Dosage:10 mg/kg
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Administration:i.v.; single dose
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Result:Reported AUC(0-t) of 255.53 mg/L*h, T1/2 of 1.43 h, Tmax of 0.5 h, VZ of 0.08 L/kg, CLZ of 0.04 L/h/kg, and Cmax of 73.93 mg/L.
Chemical Information
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Peso molecular 1725.76
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Fòrmula C78H104N18O27
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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)
CLP-d2 Related Classifications
HY-P11617 Related Classifications
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