阿莫地喹盐酸盐 T0381

Product Introduction
Bioactivity


英文名: Amodiaquine dihydrochloride dihydrate

描述: Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) 是一种具有口服活性的组胺 N-甲基转移酶抑制剂，也是一种Nurr1激动剂，可特异性结合Nurr1的配体结合域，EC50约为20 μM。它是 4-氨基喹啉衍生物，具有抗疟和抗炎特性。

激酶实验: Whole-cell competitive binding assays: Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with 18F-FDHT, increasing concentrations (1pM to 1 μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of 18F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R2 > 0.99.

体内活性: 在体内给予小剂量的 Amodiaquine dihydrochloride dihydrate 对狗的胃液分泌具有显著增效作用，能显著增强组胺的效应[3]。Amodiaquine dihydrochloride dihydrate 能够预防由P. acnes诱导和LPS加剧的严重肝损伤，且治疗可增强这类小鼠肝脏内组胺水平的升高而不伴随远端甲基组胺的增高[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 85 mg/mL (182.9 mM)
H2O : 27 mg/mL (58.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: antimalarial | anti-inflammatory | CXCL2 | CCL2 | N-methyltransferase | neuroprotective | Amodiaquin dihydrochloride Dihydrate | Inhibitor | Amodiaquine | Amodiaquine Hydrochloride | Amodiaquine dihydrochloride dihydrate | Parasite | Amodiaquine dihydrochloride Dihydrate | IL-1β | Nurr1 | Histone Methyltransferase | inhibit | Amodiaquin

相关产品: BCI-121 | PRMT5-IN-25 | EZM0414 | DW14800 | MI-463 | Antitumor agent-101 | PRMT5-IN-31 | JQEZ5 | XY1 | MS37452

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Metabolism Disease Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Parasitic Compound Library | Anti-Fibrosis Compound Library | Chromatin Modification Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途