DZ2002|cas:33231-14-0|西域试剂

DZ2002,99.68%

产品编号：Bellancom-18620| CAS NO：33231-14-0| 分子式：C₁₀H₁₃N₅O₃| 分子量：251.24

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18620	￥2333.00	杭州北京（现货）
Bellancom-18620	￥3500.00	杭州北京（现货）
Bellancom-18620	￥5000.00	杭州北京（现货）
Bellancom-18620	￥15000.00	杭州北京（现货）
Bellancom-18620	￥21000.00	杭州北京（现货）

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DZ2002

产品介绍

DZ2002 是一种口服有效的、可逆的、低细胞毒性的 III 型 SAHH 抑制剂 (K_i=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。

生物活性

DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (K_i=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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 61 mg/mL (242.80 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9803 mL	19.9013 mL	39.8026 mL
5 mM	0.7961 mL	3.9803 mL	7.9605 mL
10 mM	0.3980 mL	1.9901 mL	3.9803 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (9.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.95 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (9.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.95 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。