产品
编 号：F136979
分子式：C26H31N7O
分子量：457.57
分子式：C26H31N7O
分子量：457.57
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1358099-18-9
产品详情
生物活性：
C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.
体内研究：
C25-140 (~1.5 mg/kg; topically to the shaved back and the right ear; twice daily for 6 days) ameliorates symptoms of autoimmune psoriasis in R 837-induced psoriasis mouse model.?C25-140 (6-14 mg/kg; given i.p.; twice daily for 14 days) shows a dose-dependent improvement of RA disease outcome in Collagen-induced arthritis (CIA) model.?C25-140 (10 mg/kg; i.v.) treatment shows that the Cmax, AUC, t1/2 and Vd are 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively..?C25-140 (10 mg/kg; p.o.) treatment shows that the Cmax, AUC, t1/2 and Vd are 3.4 μg/mL, 124034 ng min/mL, 127.33 min and 13.3 L/kg, respectively.?C25-140 (10 mg/kg; i.p.) treatment shows that the Cmax, AUC, t1/2 and Vd are 4.2μg/mL, 100000 ng min/mL, 184 min, 25.6 L/kg, respectively.Animal Model:R 837-induced psoriasis mouse model (male BALB/c mice)
Dosage:~1.5 mg/kg
Administration:Topically to the shaved back and the right ear; twice daily for 6 days
Result:Showed a dose-dependent improvement of RA disease outcome.
Animal Model:Collagen-induced arthritis (CIA) model in DBA1/J mice
Dosage:6 mg/kg, 10 mg/kg, 14 mg/kg
Administration:Given i.p.; twice daily for 14 days
Result:Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of 10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammation and structural damage.
Animal Model:BALB/C mice
Dosage:10 mg/kg
Administration:I.v. (Pharmacokinetic Analysis)
Result:The Cmax, AUC, t1/2 and Vd were 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively.
体外研究：
C25-140 dose-dependently impedes TRAF6-Ubc13 interaction.?C25-140 (10-30 μM; 2 hours) effectively reduces TRAF6-mediated ubiquitin chain formation.?C25-140 affects TNFα-induced phosphorylation of IκBα as well as NF-κB-induced target gene expression.?C25-140 efficiently inhibits IL-1β- and TNFα-mediated receptor signaling in the context of cytokine activation.
C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.
体内研究：
C25-140 (~1.5 mg/kg; topically to the shaved back and the right ear; twice daily for 6 days) ameliorates symptoms of autoimmune psoriasis in R 837-induced psoriasis mouse model.?C25-140 (6-14 mg/kg; given i.p.; twice daily for 14 days) shows a dose-dependent improvement of RA disease outcome in Collagen-induced arthritis (CIA) model.?C25-140 (10 mg/kg; i.v.) treatment shows that the Cmax, AUC, t1/2 and Vd are 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively..?C25-140 (10 mg/kg; p.o.) treatment shows that the Cmax, AUC, t1/2 and Vd are 3.4 μg/mL, 124034 ng min/mL, 127.33 min and 13.3 L/kg, respectively.?C25-140 (10 mg/kg; i.p.) treatment shows that the Cmax, AUC, t1/2 and Vd are 4.2μg/mL, 100000 ng min/mL, 184 min, 25.6 L/kg, respectively.Animal Model:R 837-induced psoriasis mouse model (male BALB/c mice)
Dosage:~1.5 mg/kg
Administration:Topically to the shaved back and the right ear; twice daily for 6 days
Result:Showed a dose-dependent improvement of RA disease outcome.
Animal Model:Collagen-induced arthritis (CIA) model in DBA1/J mice
Dosage:6 mg/kg, 10 mg/kg, 14 mg/kg
Administration:Given i.p.; twice daily for 14 days
Result:Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of 10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammation and structural damage.
Animal Model:BALB/C mice
Dosage:10 mg/kg
Administration:I.v. (Pharmacokinetic Analysis)
Result:The Cmax, AUC, t1/2 and Vd were 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively.
体外研究：
C25-140 dose-dependently impedes TRAF6-Ubc13 interaction.?C25-140 (10-30 μM; 2 hours) effectively reduces TRAF6-mediated ubiquitin chain formation.?C25-140 affects TNFα-induced phosphorylation of IκBα as well as NF-κB-induced target gene expression.?C25-140 efficiently inhibits IL-1β- and TNFα-mediated receptor signaling in the context of cytokine activation.
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