产品
编 号：F323198
分子式：C10H13N5O3
分子量：251.24
分子式：C10H13N5O3
分子量：251.24
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
2mg
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5mg
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10mg
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50mg
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结构图
CAS No: 33231-14-0
产品详情
生物活性：
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 dermal thickness in BLM-induced mice.Significantly reduced collagen accumulation and α-SMA expression in the dermis of mice and suppressed the mRNA expression of vascular endothelial growth factor (VEGF) in mice skin tissue.Notably reduced collagen content and mRNA expression of the Col1a1 and Col1a2 while promoting that of the matrix metalloproteinase-13 (MMP-13) in the lesional skin of BLM-induced mice.
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.
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 dermal thickness in BLM-induced mice.Significantly reduced collagen accumulation and α-SMA expression in the dermis of mice and suppressed the mRNA expression of vascular endothelial growth factor (VEGF) in mice skin tissue.Notably reduced collagen content and mRNA expression of the Col1a1 and Col1a2 while promoting that of the matrix metalloproteinase-13 (MMP-13) in the lesional skin of BLM-induced mice.
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.
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