DPP-1-IN-2
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.
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- Formule: C18H19N5O
- Masse moléculaire:321.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
DPP-1-IN-2 potently inhibits recombinant human DPP-I enzymatic activity with an IC50 of 36.8 ± 1.9 nM[1].
DPP-1-IN-2 exhibits high selectivity for DPP-I, with only weak inhibitory activity against cathepsin K (IC50 = 18.2 ± 3.2 μM) and no activity against cathepsin L, cathepsin S, NE, PR3, or Cat G (IC50 > 50 μM)[1].
DPP-1-IN-2 potently inhibits LPS-induced NO production in RAW 264.7 macrophages with an IC50 of 0.8 ± 0.1 μM[1].
DPP-1-IN-2 (5-15 μM; 2 h) directly engages with intracellular DPP-I in U937 cells, enhancing its thermal stability in a dose-dependent manner[1].
DPP-1-IN-2 (1.25-10.00 μM; 24 h post-LPS stimulation) dose-dependently inhibits LPS-induced production of IL-1β, IL-6, TNF-α, GM-CSF, MCP-1, and CXCL2 in RAW 264.7 macrophages[1].
DPP-1-IN-2 (1.25-5.00 μM; 5 consecutive days, with daily medium refreshment and compound re-treatment) dose-dependently inhibits intracellular DPP-I, NE, PR3, and Cat G activities in U937 cells, with near-complete DPP-I inhibition at 5 μM after 5 days of treatment[1].
DPP-1-IN-2 (5 μM; 24-120 h) reduces NE, PR3, and Cat G protein levels in U937 cells in vitro in a time-dependent manner, with significant depletion observed after 48 h of continuous 5 μM treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human U937 cells
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Concentration:5 μM
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Incubation Time:24, 48, 72, 96, 120 h
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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.
DPP-1-IN-2 (10-30 mg/kg; p.o.; daily; 15 days) exerts a dose-dependent anti-inflammatory effect in adjuvant-induced arthritis rats; among these regimens, the daily dose of 30 mg/kg significantly reverses joint inflammation, reduces pro-inflammatory cytokine levels, and inhibits serum DPP-I activity to approximately 17% of the control level within 15 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (6-8 weeks old, ~20 g, balanced sex ratio)[1]
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Dosage:0.3 mg/kg; 3 mg/kg; 30 mg/kg
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Administration:p.o.; daily; 10 days
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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.
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Animal Model:Sprague-Dawley (4-week-old male, 120-130 g, adjuvant-induced arthritis model)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; daily; 15 days
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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.
Chemical Information
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Masse moléculaire 321.38
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Formule C18H19N5O
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SMILES
O=C(C1=NNC(C(C)C)=C1)N[C@H](C#N)CC2=CNC3=C2C=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DPP-1-IN-2 Related Classifications
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