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。
产品描述
Amodiaquine Hydrochloride is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties.
体内活性
In vivo administration of a small dose amodiaquine dramatically enhanced the effect of histamine on the gastric secretion in dogs[3]. Amodiaquine prevents severe hepatic injury and high lethality in P. acnes-primed and LPS-induced hepatitis mice. Its treatment enhances the elevation of histamine in the liver of P. acnes-primed and LPS-induced hepatitis mice without accompanying tele-methyl histamine elevation[1].
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.
Cas No.
6398-98-7
分子式
C20H28Cl3N3O3
分子量
464.81
别名
阿莫地喹盐酸盐;Amodiaquine hydrochloride;Amodiaquin dihydrochloride dihydrate
储存和溶解度
H2O:27 mg/mL (58.1 mM)
DMSO:85 mg/mL (182.9 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years