NADPH oxidase-IN-1_product_DataBase

Bioactivity	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[1].
Invitro	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[1]。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[1]。NADPH oxidase-IN-1 (10 μM; 24 h) 抑制 BV2 细胞中促炎细胞因子的 mRNA 表达[1]。NADPH oxidase-IN-1 (1 nM-10 mM; 24 h) 也抑制 BV2 细胞的激活和迁移[1]。 RT-PCR[1] Cell Line:
In Vivo	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[1]。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[1]。在大鼠中的药代动力学特征Parameters
Name	NADPH oxidase-IN-1
CAS	2762405-17-2
Formula	C20H27N3O2S
Molar Mass	373.51
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Shim S, et al. Discovery of a NADPH oxidase inhibitor,(E)-3-cyclohexyl-5-(4-((2-hydroxyethyl)(methyl) amino) benzylidene)-1-methyl-2-thioxoimidazolidin-4-oneone, as a novel therapeutic for Parkinson's disease[J]. European Journal of Medicinal Chemistry, 2022, 244: 114854.

PeptideDB

NADPH oxidase-IN-1

CAS: 2762405-17-2 F: C20H27N3O2S W: 373.51