2. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel NF-κB Immunology/Inflammation
  3. Phosphodiesterase (PDE) TRP Channel NF-κB NOD-like Receptor (NLR) Interleukin Related
  4. 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.

For research use only. We do not sell to patients.

Multitarget AD-IN-6

Multitarget AD-IN-6 Chemical Structure

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Multitarget AD-IN-6 Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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[1].

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.

Multitarget AD-IN-6 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human bronchial smooth muscle cells (BSMC)
Concentration: 10-50 μM
Incubation Time: 48 h
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

Multitarget AD-IN-6 (25 mg/kg; i.p.; 14 days) significantly attenuates elastase-induced COPD pathology in mice, including air space enlargement, lung inflammation, NLRP3 inflammasome activation, and NF-κB phosphorylation[1].

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

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]
Dosage: 25 mg/kg
Administration: i.p.; once daily; 14 consecutive days
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.
Molecular Weight

547.61

Formula

C28H33N7O5
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Multitarget AD-IN-6 Related Classifications

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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:

Multitarget AD-IN-6Phosphodiesterase (PDE)TRP ChannelNF-κBNOD-like Receptor (NLR)Interleukin RelatedTransient receptor potential channelsNuclear factor-κBNuclear factor-kappaBILPDE4Bchronic obstructive pulmonary diseaseTRPA1PDE7Aelastase-induced emphysema murine modelsCHIT1NLRP3 inflammasomehuman airway cell-based modelsRAW 264.7 murine macrophagesInhibitorinhibitorinhibit

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