2. 疾病领域
  3. 炎症和免疫系统疾病 肌肉骨骼疾病
  4. 自身免疫性疾病 关节炎
  5. 类风湿性关节炎
  6. DPP-1-IN-2

DPP-1-IN-2 是一种 DPP-I 抑制剂，对人源 IC50 为 36.8 nM，且具有口服有效性。DPP-1-IN-2 可与细胞内的 DPP-I 结合，提高其热稳定性，并通过抑制其酶活性来降低下游中性粒细胞丝氨酸蛋白酶的活性与表达水平。DPP-1-IN-2 可调控炎症因子与趋化因子的分泌，从而发挥抗炎作用。DPP-1-IN-2 可逆转佐剂诱导的关节炎大鼠模型中的关节炎症与组织损伤。DPP-1-IN-2 可用于关节炎的相关研究。

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DPP-1-IN-2

DPP-1-IN-2 Chemical Structure

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DPP-1-IN-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DPP-1-IN-2 is a DPP-I inhibitor with a human IC50 of 36.8 nM and oral efficacy. DPP-1-IN-2 binds to intracellular DPP-I, increases its thermal stability, and reduces the activity and expression levels of downstream neutrophil serine proteases by inhibiting its enzymatic activity. DPP-1-IN-2 regulates the secretion of inflammatory factors and chemokines to exert anti-inflammatory effects. DPP-1-IN-2 reverses joint inflammation and tissue damage in adjuvant-induced arthritis rat models. DPP-1-IN-2 is applicable to research related to arthritis[1].

体外研究
(In Vitro)

DPP-1-IN-2 (Compound C10b) 可强效抑制重组人 DPP-I 的酶活性，其 IC50 为 36.8 nM[1]。
DPP-1-IN-2 对 DPP-I 具有高选择性，对组织蛋白酶 K 仅表现出微弱的抑制活性 (IC50 = 18.2 μM)，而对组织蛋白酶 L、组织蛋白酶 S、NE、PR3 或 Cat G 无抑制活性 (IC50 > 50 μM)[1]。
DPP-1-IN-2 可强效抑制 LPS (HY-D1056) 诱导的 RAW 264.7 巨噬细胞中 NO 的生成，其 IC50 为 0.8 μM[1]。
DPP-1-IN-2 (5-15 μM; 2 h) 可直接与 U937 细胞内的细胞内 DPP-I 结合，并以剂量依赖的方式提高其热稳定性[1]。
DPP-1-IN-2 (1.25-10.00 μM; 24 h post-LPS stimulation) 可呈剂量依赖性抑制 LPS 诱导的 RAW 264.7 巨噬细胞中 IL-1β、IL-6、TNF-α、GM-CSF、MCP-1 和 CXCL2 的产生[1]。
DPP-1-IN-2 (1.25-5.00 μM; 5 consecutive days, with daily medium refreshment and compound re-treatment) 可剂量依赖性地抑制 U937 细胞内的 DPP-I、NE、PR3 和 Cat G 活性，在 5 μM 浓度下处理 5 天后可近乎完全抑制 DPP-I 活性[1]。
DPP-1-IN-2 (5 μM; 24-120 h) 可在体外以时间依赖的方式降低 U937 细胞中 NE、PR3 和 Cat G 的蛋白水平，持续以 5 μM 处理 48 h 后可观察到显著的蛋白消耗[1]。

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

DPP-1-IN-2 相关抗体:

Western Blot Analysis[1]

Cell Line: Human U937 cells
Concentration: 5 μM
Incubation Time: 24, 48, 72, 96, 120 h
Result: Reduced NE, PR3, and Cat G protein levels in a time-dependent manner.
Maintained protein levels at ~85% of initial levels after 24 h.
Dropped levels to 32.7% (NE), 38.2% (PR3), and 45.3% (Cat G) of initial levels after 72 h.
Dropped levels to 9.8% (NE), 11.8% (PR3), and 20.3% (Cat G) of initial levels after 120 h.
体内研究
(In Vivo)

DPP-1-IN-2 (0.3-30 mg/kg; p.o.; daily; 10 days) 可呈剂量依赖性抑制 C57BL/6 小鼠体内的 DPP-I 和 NSP 活性，其中每日 30 mg/kg 的剂量可产生强效抑制作用[1]。
DPP-1-IN-2 (10-30 mg/kg; p.o.; daily; 15 days) 可在佐剂诱导性关节炎大鼠中发挥剂量依赖性抗炎作用；其中每日 30 mg/kg 的剂量可在 15 天内显著逆转关节炎症、降低促炎细胞因子水平，并将血清 DPP-I 活性抑制至对照组水平的约 17%[1]。

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

Animal Model: C57BL/6 (6-8 weeks old, ~20 g, balanced sex ratio)[1]
Dosage: 0.3 mg/kg; 3 mg/kg; 30 mg/kg
Administration: p.o.; daily; 10 days
Result: Maintained DPP-I and neutrophil serine protease (NSP) activities at over 90% of normal control levels at 0.3 mg/kg.
Decreased activity levels of DPP-I and NSPs significantly compared to controls at 3 mg/kg.
Maintained DPP-I activity in blood/bone marrow at approximately 13.5%/23.5% of control levels, NE activity at 18.9%/24.9% of control levels, PR3 activity at 23.8%/30.6% of control levels, and Cat G activity at 30.5%/38.8% of control levels at 30 mg/kg.
Showed no obvious adverse reactions, mortality, significant body weight fluctuations, or pathological changes in major organs (heart, liver, spleen, lung, kidney) on H&E staining across all doses.
Animal Model: Sprague-Dawley (4-week-old male, 120-130 g, adjuvant-induced arthritis model)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; daily; 15 days
Result: Showed gradual body weight recovery starting from day 16 compared to model group rats, with the 30 mg/kg group exhibiting the most significant recovery.
Reduced paw swelling volume and arthritis index scores continuously from day 16 to day 28; the 30 mg/kg group had significantly lower scores than the model group by the end of the study.
Showed significantly reduced inflammatory cell infiltration in ankle joints, decreased local joint inflammation damage, and alleviated articular cartilage damage in the 30 mg/kg group compared to the model group via H&E and Safranin O/Fast Green staining.
Reduced levels of IL-1β, TNF-α, MCP-1, and CXCL2 in a dose-dependent manner, with the 30 mg/kg group showing significant reduction compared to the model group (magnitude comparable to the positive control).
Showed no significant reduction in serum DPP-I or NSP activities in the 10 mg/kg group; reduced serum activity levels of DPP-I, NE, PR3, and Cat G to approximately 17%, 22%, 30%, and 35% of control group levels, respectively, in the 30 mg/kg group.
分子量

321.38

Formula

C18H19N5O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DPP-1-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DPP-1-IN-2OthersRAW 264.7 macrophagesadjuvant-induced arthritisneutrophil serine proteaseDPP-Iratcathepsin Scathepsin Kcathepsin LU937 cellsC57BL/6 miceInhibitorinhibitorinhibit

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