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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50 mg | ¥ 236 | 现货 | |
100 mg | ¥ 413 | 现货 | |
200 mg | ¥ 588 | 现货 | |
500 mg | ¥ 980 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 163 | 现货 |
产品描述 | Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties. |
靶点活性 | Histamine N-methyl transferase:18.6 nM(Ki) |
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]。 |
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. |
别名 | 阿莫地喹盐酸盐, Amodiaquine hydrochloride, Amodiaquin dihydrochloride dihydrate |
分子量 | 464.82 |
分子式 | C20H28Cl3N3O3 |
CAS No. | 6398-98-7 |
Smiles | O.Cl.CCN(CC)Cc1c(O)ccc(Nc2c3ccc(Cl)cc3ncc2)c1.O.Cl |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 85 mg/mL (182.9 mM) H2O: 27 mg/mL (58.1 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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