产品
编 号：F755661
分子式：C20H27N3O2S
分子量：373.51
分子式：C20H27N3O2S
分子量：373.51
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 2762405-17-2
产品详情
生物活性：
NADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy.
体内研究：
NADPH oxidase-IN-1 (化合物11) (30 mg/kg; 口服给药; 每日给药, 共 4 周) 在患帕金森疾病的小鼠模型中，能够减弱 MPTP 诱导的小胶质细胞激活，减少多巴胺能神经元损伤。NADPH oxidase-IN-1 通过静脉注射 (10-300 mg/kg; 单次给药) 和灌胃 (10- 1000mg /kg;单次剂量) 处理，对雄性和雌性小鼠都是安全的。在大鼠中的药代动力学特征ParametersC0 (μg/mL)Cmax (μg/mL)t1/2 (h)Tmax (h)AUClast (μg/h/mL)ke (1/h)Vd (L)Vd/F (L)Cl (L/h)Cl/F (L/h)F (%)
IV (2 mg/kg)1.700.790.4681.320.2110.217
PO (10 mg/kg)0.6095.01[0.083-2]1.310.1701.990.34156.0
PO (20 mg/kg)0.7836.13[0.67-2]4.160.1591.820.21788.9
体外研究：
NADPH oxidase-IN-1 (化合物11) 可以穿过血脑屏障，Pe 值为 13.6 (10-6 cm/s)，由平行人工膜透性试验 (PAMPA) 测定。NADPH oxidase-IN-1 (1 nM-10 mM; 30min) 抑制 LPS 诱导 BV2 小胶质细胞产生 ROS，并呈剂量依赖性。NADPH oxidase-IN-1 (10 μM; 24 h) 抑制 BV2 细胞中促炎细胞因子的 mRNA 表达。NADPH oxidase-IN-1 (1 nM-10 mM; 24 h) 也抑制 BV2 细胞的激活和迁移。
NADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy.
体内研究：
NADPH oxidase-IN-1 (化合物11) (30 mg/kg; 口服给药; 每日给药, 共 4 周) 在患帕金森疾病的小鼠模型中，能够减弱 MPTP 诱导的小胶质细胞激活，减少多巴胺能神经元损伤。NADPH oxidase-IN-1 通过静脉注射 (10-300 mg/kg; 单次给药) 和灌胃 (10- 1000mg /kg;单次剂量) 处理，对雄性和雌性小鼠都是安全的。在大鼠中的药代动力学特征ParametersC0 (μg/mL)Cmax (μg/mL)t1/2 (h)Tmax (h)AUClast (μg/h/mL)ke (1/h)Vd (L)Vd/F (L)Cl (L/h)Cl/F (L/h)F (%)
IV (2 mg/kg)1.700.790.4681.320.2110.217
PO (10 mg/kg)0.6095.01[0.083-2]1.310.1701.990.34156.0
PO (20 mg/kg)0.7836.13[0.67-2]4.160.1591.820.21788.9
体外研究：
NADPH oxidase-IN-1 (化合物11) 可以穿过血脑屏障，Pe 值为 13.6 (10-6 cm/s)，由平行人工膜透性试验 (PAMPA) 测定。NADPH oxidase-IN-1 (1 nM-10 mM; 30min) 抑制 LPS 诱导 BV2 小胶质细胞产生 ROS，并呈剂量依赖性。NADPH oxidase-IN-1 (10 μM; 24 h) 抑制 BV2 细胞中促炎细胞因子的 mRNA 表达。NADPH oxidase-IN-1 (1 nM-10 mM; 24 h) 也抑制 BV2 细胞的激活和迁移。
产品资料
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