化合物DZ2002 T11134

Product Introduction
Bioactivity


英文名: DZ2002

描述: DZ2002 是一种口服有效的、可逆的、低细胞毒性的 III 型 SAHH 抑制剂 (Ki=17.9 nM)，具有较好的免疫抑制活性。DZ2002 能通过逆转各种细胞类型的促纤维化表型来防止实验性皮肤纤维化的发展。DZ2002 可用于自身免疫性疾病，如狼疮综合征和系统性硬化症的研究。

体外活性: DZ2002 (0.1, 1, 10 µM; 96 h) inhibits the mixed lymphocyte reaction (MLR) response. DZ2002 (0.1, 1, 10 µM; 24 h) inhibits IL-12 and TNF-α production from both mouse peritoneal exudate cells and humanTHP-1 Cells. DZ2002 (0.1, 1, 10 µM; 64 h) inhibits expression of B7 (CD80/CD86) on differentiated THP-1 cells[1].

体内活性: DZ2002 (2, 10, 50 mg/kg; i.p.; twice) blocks the DNFB-induced DTH response. (DNFB-induced DTH is a Th1 cell-mediated immune response, in which IL-12 is highly expressed and macrophages have been shown to play an important role). DZ2002 (0.08, 2 mg/kg; i.p.; single daily for 7 days) significantly suppresses a delayed-type hypersensitivity reaction as well as antibody secretion[1]. DZ2002 (50, 100 mg/kg; p.o.; single daily for 4 weeks) exerts a potent anti-fibrotic effect on dermal fibrosis by reducing the production of collagen, facilitating its degradation and regulating expression of various soluble factors in SSc mice model[2].

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

溶解度: DMSO : 54.9mg/mL (218.5mM)


关键字: DZ-2002 | DZ 2002 | DZ2002

相关库: Bioactive Compounds Library Max | Bioactive 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