Multitarget AD-IN-6
Multitarget AD-IN-6 (Compound 39) is a multi-target inhibitor, with an IC50 of 15.54 μM against PDE4B, 15.15 μM against PDE7A, 8.39 μM against PDE3A, and a Kd of 37.7 μM against CHIT1. Multitarget AD-IN-6 acts as a TRPA1 antagonist, reduces the level of the NLRP3 inflammasome multiprotein complex to inhibit its activation, while inhibiting PDE4B, PDE7A and CHIT1, and decreasing the phosphorylation of NF-κB. Multitarget AD-IN-6 improves the pathology of elastase-induced emphysema in mice. Multitarget AD-IN-6 is applicable for the research of chronic obstructive pulmonary disease.
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- Fòrmula: C28H33N7O5
- Peso molecular:547.61
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Descripciòn
IC50 & Target
[1]|
PDE4B 15.54 μM (IC50) |
PDE7A 15.15 μM (IC50) |
PDE1B 54.47 μM (IC50) |
PDE2A 79.61 μM (IC50) |
PDE3A 8.39 μM (IC50) |
hPDE4D 130.50 μM (IC50) |
PDE5A 26.86 μM (IC50) |
PDE8A 16.46 μM (IC50) |
human PDE 10A 36.13 μM (IC50) |
TRPA1 |
IL-6 |
In Vitro
Multitarget AD-IN-6 inhibits recombinant human PDE4B with an IC50 of 15.54 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE7A with an IC50 of 15.15 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE1B with an IC50 of 54.47 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE2A with an IC50 of 79.61 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE3A with an IC50 of 8.39 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE4D with an IC50 of 130.50 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE5A with an IC50 of 26.86 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE8A with an IC50 of 16.46 μM[1].
Multitarget AD-IN-6 inhibits recombinant human PDE10A with an IC50 value of 36.13 μM[1].
Multitarget AD-IN-6 (100 μM) acts as an antagonist of the TRPA1 channel, inhibiting 51% of its activity at a concentration of 100 μM without agonist effects[1].
Multitarget AD-IN-6 inhibits recombinant human CHIT1 with an inhibition rate of 57% and a Kd value of 37.7 μM[1].
Multitarget AD-IN-6 (10 μM; 1 h) inhibits LPS-induced production of nitric oxide, TNF-α, and IL-6 in RAW 264.7 mouse macrophages, exhibiting anti-inflammatory activity[1].
Multitarget AD-IN-6 (10-50 μM; 48 h) reduces fetal bovine serum (FBS)-induced proliferation of bronchial smooth muscle cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human bronchial smooth muscle cells (BSMC)
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Concentration:10-50 μM
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Incubation Time:48 h
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Result:Reduced FBS-induced BSMC proliferation by 38% relative to untreated cells at 10 μM.
Further reduced BSMC proliferation in a concentration-dependent manner at 50 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 8-10 weeks old, mean weight 25.5 g, intranasally instilled with porcine pancreatic elastase 4 times weekly for 21 days to induce emphysema)[1]
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Dosage:25 mg/kg
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Administration:i.p.; once daily; 14 consecutive days
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Result:Reduced mean linear intercept (MLI) from 59.50 μm to 50.36 μm, attenuating elastase-induced air space enlargement.
Significantly reduced the total number of inflammatory cells in BALF in both acute and chronic experimental settings; in the acute model, this effect was stronger than that of roflumilast.
Normalized PPE-induced elevated transcript levels of pro-inflammatory genes *Tnfa*, *Cxcl2*, *Il6*, and *Il1b* in lung homogenates to control levels.
Reduced PPE-induced increases in NLRP3, ASC/TMS1, and cleaved caspase-1 protein levels in lung homogenates to match control levels.
Decreased PPE-induced NF-κB p65 phosphorylation in lung homogenates to control levels.
Chemical Information
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Peso molecular 547.61
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Fòrmula C28H33N7O5
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SMILES
CC(C)(C)OC(C1=CC=C(NC(CCCN2C(C(N(C)C(N3C)=O)=O)=C3N=C2NCC4=NC=CC=C4)=O)C=C1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Multitarget AD-IN-6 Related Classifications
HY-181762 Related Classifications
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