2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. MMP Interleukin Related
  4. ADAM17-IN-1

ADAM17-IN-1 是一种选择性 ADAM17 抑制剂。ADAM17-IN-1 通过抑制 ADAM17 活性以降低树突状细胞 (DCs) 的代谢活性，削弱 DC 抗原呈递功能，抑制过敏原特异性 Th2 细胞极化，并减少 Th2 细胞因子 (IL-4、IL-5、IL-13) 的分泌。ADAM17-IN-1 在小鼠屋尘螨 (HDM) 诱导的 2 型/嗜酸性粒细胞性气道炎症中表现出保护效应。ADAM17-IN-1 可用于 2 型高反应性过敏性哮喘的研究。

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ADAM17-IN-1

ADAM17-IN-1 Chemical Structure

CAS No. : 1802395-34-1

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ADAM17-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ADAM17-IN-1 is a selective inhibitor of ADAM17. ADAM17-IN-1 inhibits ADAM17 activity to reduce metabolic activity of dendritic cells (DCs), impair DC antigen-presenting function, suppress allergen-specific Th2 cell polarization, and reduce Th2 cytokine (IL-4, IL-5, IL-13) secretion. ADAM17-IN-1 demonstrates protective efficacy against house dust mite (HDM)-induced type 2/eosinophilic airway inflammation in mice. ADAM17-IN-1 can be used for the study of type 2-high allergic asthma[1].

IC50 & Target[1]

ADAM17

 

体外研究
(In Vitro)

ADAM17-IN-1 (Compound 2155-17) (50 μM) 显著降低 BMDCs 的氧消耗率 (OCR) 和储备呼吸能力 (SRC)，抑制线粒体氧化磷酸化，并损伤 DC 代谢活性[1]。
ADAM17-IN-1 (50 μM, 预处理 HDM 刺激的 BMDCs 后与 OTII 小鼠来源的 CFSE 标记 CD4+T 细胞共培养 4 天) 显著降低 OVA323-339 肽特异性 T 细胞增殖率，减少 Th2 细胞因子 (IL-13) 分泌及 CD4+GATA3+Th2 细胞比例[1]。
ADAM17-IN-1 (0.316-3.16 μM, 处理小鼠少突胶质细胞前体 (OPCs)) 以剂量依赖方式促进 OPC 分化，不诱导细胞凋亡，且未显示明显细胞毒性[1]。

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

ADAM17-IN-1 相关抗体:
体内研究
(In Vivo)

ADAM17-IN-1 (Compound 2155-17) (体外预处理 50 μM，16 小时，采用 0.75×105 CD11c+ BMDCs 通过鼻内给药在第 0 天进行转移，随后在第 9、11、13、15 天进行 HDM 挑战 (50 μg/只小鼠)) 显著降低 BAL 和肺组织中的嗜酸性粒细胞数量[1]。
ADAM17-IN-1 (200 μg/只小鼠，鼻内给药，第 8、10、12、14 天与 HDM 激发同时进行) 显著减少 BAL/肺中的总炎症细胞和嗜酸性粒细胞数量[1]。

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

Animal Model: HDM-induced allergic asthma model in WT mice (C57BL/6, 6-10 weeks old) with adoptive transfer of BMDCs[1]
Dosage: 50 μM in vitro pre-treatment for 16 h
Administration: Adoptive transfer of 0.75×105 CD11c+ BMDCs via i.n. on Day 0, followed by i.n. HDM challenge (50 μg/mouse) on Days 9, 11, 13, 15
Result: Exhibited decreased number of total BAL cells and eosinophils.
Reduced BAL CCL24 levels and serum HDM-specific IgG1/IgE levels.
Declined IL4, IL5, and IL13 production in DLn cells.
Alleviated peribronchial inflammatory cell infiltrates and mucous cell metaplasia in lung.
Animal Model: HDM-induced allergic asthma model in WT mice (C57BL/6, 6-10 weeks old) with adoptive transfer of BMDCs[1]
Dosage: 200 μg/mouse
Administration: i.n., Days 8, 10, 12, 14 concurrent with HDM challenge
Result: Reduced total inflammatory cells and eosinophils in BAL and lung.
Decreased serum HDM-specific IgG1/IgE levels and lung IL5/IL13 levels.
Reduced peribronchial inflammatory cell infiltrates and mucous cell metaplasia in lung.
分子量

669.90

Formula

C40H55N5O4
CAS 号
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

ADAM17-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

ADAM17-IN-11802395-34-1MMPInterleukin RelatedMatrix metalloproteinasesILADAM17Airway inflammationAsthmaDendritic cellTh2 immunityAllergyInhibitorinhibitorinhibit

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