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Tak 242

Manufactured by R&D Systems
Sourced in United States

TAK-242 is a small molecule inhibitor that targets the Toll-like receptor 4 (TLR4) signaling pathway. It acts as an antagonist of TLR4, which plays a crucial role in the innate immune response. The core function of TAK-242 is to inhibit TLR4-mediated signaling, which can be used in research applications.

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5 protocols using tak 242

1

Inhibition of Inflammatory Pathways

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TAK-242 (CAS 243984-11-4 Cat 6587/5) was from R&D Systems (Minneapolis MN). LPS-RS (from Rhodobacter sphaeroides, Catalog # tlrl-rslps) and MCC950 (CAS 210826-40-7, Catalog # inh-mcc) were purchased from InvivoGen (San Diego CA). Other chemicals, including minocycline (CAS 13614-98-7, Cat# M2280000) and IL1-Ra (Cat# SRP 3084), and salts were obtained from Millipore Sigma Chemical Company. Drugs were prepared as stock solutions in either ACSF or DMSO and diluted to final concentration at the time of experiment. The concentrations of TAK-242, LPS-RS and minocycline are based on our previous studies using those inhibitors against LPS23 . The dose and concentrations of MCC950 and IL1-Ra followed studies by Coll et al.14 (link) and Edy et al.25 (link), respectively.
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2

Inhibition of Mycobacterial-Induced Inflammation

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Heat-killed mycobacterium tuberculosis was purchased from InvivoGen (San Diego, CA, USA). The Met5A cells and mouse PMCs were treated with 10 ng/mL HKMT either with or without inhibitors for the time periods indicated. The PD98059 (MEK inhibitor), losartan (AT1R antagonist), and TAK-242 (TLR4 inhibitor) were purchased from R&D Systems (Minneapolis, MN, USA). To suppress endogenous NOX4 expression, a specific siRNA (BioneerInc, Daejeon, Korea) against NOX4 based on the target region from the NOX4 gene (sense: 5′-UCAGACAAAUGUAGACAC-3′ and antisense: 5′-AGUGUCUACAUUUGUCUG-3′) was used in experiments. Scrambled siRNA (sense: 5′-GGTCAAGACACTATTAACA-3′ and antisense: 5′-GGATTCCTAGTGTATTTCA-3′) was used as a control (SiCon).
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3

Inhibitor Compounds for Inflammation Studies

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TAK-242 (CAS 243984-11-4 Cat 6587) was purchased from R&D Systems (Minneapolis MN). Lipopolysaccharide from Rhodobacter sphaeroides (LPS-RS) (Catalog # tlrl-rslps) and MCC950 (CAS 210826-40-7, Catalog # inh-mcc) were purchased from InvivoGen (San Diego CA). Trans-ISRIB (CAS 1597403-47-8, Cat 5284) was from Tocris (Ellisville MO). Other chemicals, including glyphosate (CAS 1071-83-6), minocycline (CAS 13614-98-7, Cat# M2280000) and IL1-Ra (Cat# SRP 3084), quercetin (CAS 849061-97-8, PHR1488) and salts were obtained from Millipore Sigma Chemical Company. Roundup, a herbicide containing glyphosate, was purchased from a local store. Drugs were prepared as stock solutions in either ACSF or DMSO and diluted to final concentration at the time of experiment. The concentrations of TAK-242, LPS-RS and minocycline are based on our previous studies using those inhibitors against lipopolysaccharide (LPS) and acrylamide21 (link),22 (link). The concentrations of MCC950 were also based on our previous paper22 (link). The dose of TAK-242 in the behavioral study followed a proceeding report by Ono et al.30 (link).
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4

Intrathecal Infusion of Pharmacological Agents in Rats

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A total of 120 rats were randomly assigned to the following groups via a random number table: sham, IR, IR + CXCL12-neutralizing antibody (IR + N), IR + control IgG (IR + C), antibody IR + CXCR4 antagonist (AMD3100, IR + A), and IR + TLR4 inhibitor (TAK-242, I/R + T).
In all groups, we used a microsyringe to intrathecally infuse 10 μl of normal saline, 20 μg/10 μl of CXCL12-neutralizing antibody (R&D Systems, USA), 10 μg/10 μl of control IgG antibody (R&D Systems, USA), 10 μg/10 μl of CXCR4-specific antagonist (AMD3100, EMD Millipore, USA) or 30 μg/10 μl of TAK-242 (EMD Millipore, USA). All drug doses were based on the results of preliminary experiments. Intrathecal infusions were administered for 5 consecutive days before surgery, and neurological signs were assessed after each injection. Only the rats with normal motor and sensory function were included in the follow-up experiments.
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5

TLR4 Antagonist-Mediated Neuroprotection

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TAK-242 (CAS 243984-11-4 Cat 6587) was purchased from R&D Systems (Minneapolis MN). Lipopolysaccharide from Rhodobacter sphaeroides (LPS-RS) (Catalog # tlrl-rslps) and MCC950 (CAS 210826-40-7, Catalog # inh-mcc) were purchased from InvivoGen (San Diego CA). Trans-ISRIB (CAS 1597403-47-8, Cat 5284) was from Tocris (Ellisville MO). Other chemicals, including glyphosate (CAS 1071-83-6), minocycline (CAS 13614-98-7, Cat# M2280000) and IL1-Ra (Cat# SRP 3084), quercetin (CAS 849061-97-8, PHR1488) and salts were obtained from Millipore Sigma Chemical Company. Roundup, a herbicide containing glyphosate, was purchased from a local store. Drugs were prepared as stock solutions in either ACSF or DMSO and diluted to final concentration at the time of experiment. The concentrations of TAK-242, LPS-RS and minocycline are based on our previous studies using those inhibitors against lipopolysaccharide (LPS) and acrylamide (Izumi, Cashikar, et al., 2021 (link); Izumi et al., 2022 (link)). The concentrations of MCC950 were also based on our previous paper (Izumi et al., 2022 (link)). The dose of TAK-242 in the behavioral study followed a proceeding report by Ono et al. (Ono et al., 2020 (link)).
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