产品
编 号:F757192
分子式:C26H28FN5O
分子量:445.53
产品类型
结构图
CAS No: 3000541-95-4
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生物活性:
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model.
体内研究:
ROCK2-IN-7(20-80 mg/kg,口服,连续 7 天) 降低与 IL-23/Th17 轴相关的关键白细胞介素和参与角质形成细胞增殖的重要因子。ROCK2-IN-79(20-80 mg/kg,口服,连续 7 天) 抑制全身免疫激活,减轻炎症。Animal Model:IMQ-induced skin inflammation
Dosage:20 mg/kg , 40 mg/kg, 80 mg/kg
Administration:Oral gavage (p.o.)
Result:Decrease the mRNA levels of interleukin (IL)-17A, IL-17F, IL-22, and IL-23.Decreased phosphorylation of STAT3.Attenuated psoriasis-like symptoms including invasive erythema, roughness, swelling, and scales. Reduced the spleen index. Reduced the number of IL-17A+ cells.Reduced the number of cells positive for phosphorylated signal transducers and activators of transcription 3 (pSTAT3) and transcription 5 (pSTAT5). Reversed the thickening of the epidermis.Decreased the number of Ki67+ cells.
体外研究:
ROCK2-IN-7 (2-5 μM, 24 小时) 在 HaCaT 细胞中抑制 ROCK2/pSTAT3 信号通路。