| 产品描述： | DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis |
| 体外研究： |
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. Cell Proliferation Assay Cell Line: BALB/c and C57BL/6 splenocytes (Mitomycin C-pretreated; mixed lymphocyte) Concentration: 0.1, 1, 10 µM Incubation Time: 96 h Result: Suppressed the MLR by 24.5, 42.3, and 46.0% at dosages of 0.1, 1, and 10 µM, respectively. Cell Viability Assay Cell Line: TG-stimulated mouse peritoneal macrophages and human THP-1 cells Concentration: 0.1, 1, 10 µM Incubation Time: 24 h Result: Significantly blocked IL-12 p40 production from ~1800 pg/mL in untreated cells to ~850 pg/ml at 10 µM, and drastically reduced the active p70 form from ~1200 pg/mL in untreated cells to ~50 pg/mL.Reduced TNF-α level by 45%. Cell Viability Assay Cell Line: THP-1 cells Concentration: 0.1, 1, 10 µM Incubation Time: 64 h Result: Dramatically down-regulated CD80 and, in particular, CD86 expression in a dose-dependent manner. |
| 体内研究： |
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. 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. Animal Model: Male and female BALB/c and C57BL/6 mice (6 to 8-week-old; DNFB-induced ear swelling model). Dosage: 2, 10, 50 mg/kg Administration: Intraperitoneal injection; twice (1 h before and 24 h after challenge) Result: Suppressed ear swelling by 19.1, 28.7, and 33.1%, respectively and in a dose-dependent manner. Animal Model: Male and female BALB/c and C57BL/6 mice (6 to 8-week-old; DNFB-induced ear swelling model). Dosage: 0.08, 2 mg/kg Administration: Intraperitoneal injection; single daily for 7 days. Result: Inhibited hemolysis by 24.5 and 18.4% at doses of 0.08 and 2 mg/kg, respectively, thus decreasing anti-SRBC antibody production in vivo. Animal Model: Wild-type C57BL/6 mice (8 to 12-week-old; BLM-induced mice model of SSc). Dosage: 50, 100 mg/kg Administration: Oral gavage; single daily for 4 weeks. Result: Significantly decreased skin thickness and d |
| 参考文献： |
1. Wu QL, et al. Inhibition of S-adenosyl-L-homocysteine hydrolase induces immunosuppression. J Pharmacol Exp Ther. 2005 May;313(2):705-11. 2. Zhang Z, et al. DZ2002 ameliorates fibrosis, inflammation, and vasculopathy in experimental systemic sclerosis models. Arthritis Res Ther. 2019 Dec 16;21(1):290. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.98 ml |
19.901 ml |
39.802 ml |
| 5 mM |
0.796 ml |
3.98 ml |
7.96 ml |
| 10 mM |
0.398 ml |
1.99 ml |
3.98 ml |
| 50 mM |
0.08 ml |
0.398 ml |
0.796 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京