产品
编 号：F755827
分子式：C18H18O4
分子量：298.33
分子式：C18H18O4
分子量：298.33
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CAS No: 2767124-77-4
产品详情
生物活性：
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis.
体内研究：
(R)-STU104 (1, 3 and 10 mg/kg; IG for 7 days) ameliorates the symptoms of DSS-induced experimental colitis in mice, and significantly inhibits inflammatory cytokine protein.Pharmacokinetic Parameters of (R)-STU104 in male C57 mice.IV (5 mg/kg) PO (30 mg/kg)
Tmax (h)0.083
AUC0-t (μg/L·h)72499895
AUC0-∞ (μg/L·h)863516991
MRT0-∞ (h)7.3212.52
Cmax (ng/mL)29202290
t1/2 (ng/mL)9.298.67
VZ (L/kg)7.763.68
CLZ (ng/mL)0.580.29
F (%)33%
Animal Model:C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis)
Dosage:1, 3 and 10 mg/kg
Administration:IG, for 7 days
Result:Ameliorated the symptoms of DSS-induced experimental colitis, and significantly inhibited inflammatory cytokine protein TNF-α, IL-1β, IL-6, and IL-23.
体外研究：
(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production.
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis.
体内研究：
(R)-STU104 (1, 3 and 10 mg/kg; IG for 7 days) ameliorates the symptoms of DSS-induced experimental colitis in mice, and significantly inhibits inflammatory cytokine protein.Pharmacokinetic Parameters of (R)-STU104 in male C57 mice.IV (5 mg/kg) PO (30 mg/kg)
Tmax (h)0.083
AUC0-t (μg/L·h)72499895
AUC0-∞ (μg/L·h)863516991
MRT0-∞ (h)7.3212.52
Cmax (ng/mL)29202290
t1/2 (ng/mL)9.298.67
VZ (L/kg)7.763.68
CLZ (ng/mL)0.580.29
F (%)33%
Animal Model:C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis)
Dosage:1, 3 and 10 mg/kg
Administration:IG, for 7 days
Result:Ameliorated the symptoms of DSS-induced experimental colitis, and significantly inhibited inflammatory cytokine protein TNF-α, IL-1β, IL-6, and IL-23.
体外研究：
(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production.
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