ADAM17-IN-1
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.
For research use only. We do not sell to patients.
- CAS No.: 1802395-34-1
- Formula: C40H55N5O4
- Molecular Weight:669.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ADAM17 |
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Cell Line
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Type | Value | Description | References |
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| THP-1 | IC50 |
28 μM
Compound: 19
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Inhibition of ADAM17 in human THP1 cells assessed as inhibition of LPS-stimulated TNFalpha cleavage after 1 hr by AlphaScreen assay
Inhibition of ADAM17 in human THP1 cells assessed as inhibition of LPS-stimulated TNFalpha cleavage after 1 hr by AlphaScreen assay
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[PMID: 26192023] |
ADAM17-IN-1 (Compound 2155-17) (50 μM) significantly reduces the oxygen consumption rate (OCR) and spare respiratory capacity (SRC) of BMDCs, inhibits mitochondrial oxidative phosphorylation, and impairs DC metabolic activity[1].
ADAM17-IN-1 (50 μM, pre-treated HDM-pulsed BMDCs followed by 4-day co-culture with CFSE-labeled CD4+T cells from OTII mice) significantly decreases OVA323-339 peptide-specific T cell proliferation rate, reduces Th2 cytokine (IL-13) secretion and the proportion of CD4+GATA3+Th2 cells[1].
ADAM17-IN-1 (0.316-3.16 μM, treated on mouse oligodendrocyte progenitor cells (OPCs)) promotes OPC differentiation in a dose-dependent manner without inducing cell apoptosis, showing no obvious cytotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ADAM17-IN-1 (200 μg/mouse, intranasal administration, Days 8, 10, 12, 14 concurrent with HDM challenge) significantly reduces total inflammatory cells and eosinophils in BAL/lung[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HDM-induced allergic asthma model in WT mice (C57BL/6, 6-10 weeks old) with adoptive transfer of BMDCs[1]
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Dosage:50 μM in vitro pre-treatment for 16 h
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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
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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.
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Animal Model:HDM-induced allergic asthma model in WT mice (C57BL/6, 6-10 weeks old) with adoptive transfer of BMDCs[1]
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Dosage:200 μg/mouse
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Administration:i.n., Days 8, 10, 12, 14 concurrent with HDM challenge
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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.
Chemical Information
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CAS No. 1802395-34-1
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Molecular Weight 669.90
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Formula C40H55N5O4
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SMILES
CCC[C@@H](CNC(C1=O)=O)N1C[C@H](CCC2)N2C[C@H](N3C[C@@H](N(C(C3=O)=O)CCC4=CC=CC=C4)CC5=CC=CC=C5)CC6CCCCC6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ADAM17-IN-1 Related Classifications
HY-175876 Related Classifications
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