1. Immunology/Inflammation
    Autophagy
  2. Toll-like Receptor (TLR)
    Autophagy

TAK-242 (Synonyms: Resatorvid)

Cat. No.: HY-11109 Purity: 99.95% ee.: 98.00%
Handling Instructions

TAK-242 is a potent TLR4 signaling inhibitor, selectively inhibits the TLR4-mediated production of cytokines and NO.

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

TAK-242 Chemical Structure

TAK-242 Chemical Structure

CAS No. : 243984-11-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 145 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 204 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Customer Validation

    TAK-242 purchased from MCE. Usage Cited in: J Neurochem. 2016 May;137(4):576-88.

    TAK-242 markedly inhibits the up-regulation of IRAK-M and the down-regulation of p-IRAK-1 in rHMGB1-pretreated rats underwent MCAO. WB analysis of IRAK-M and p-IRAK-1 in rat ipsilateral hemispheres.

    TAK-242 purchased from MCE. Usage Cited in: Oncol Lett. 2016 Aug;12(2):1034-1040.

    Involvement of TLR4 signaling pathway in HIF-1α silencing affects inflammatory and apoptosis under hypoxic conditions. In total, 30 mg total lysate is harvested with radioimmunoprecipitation assay buffer to detect TLR4, HIF-1α, caspase-3, MyD88, p-ASK1 and p-p38 protein expression by western blot analysis in human hepatocellular carcinoma HepG2 cells. The expression of TLR4, HIF-1α, MyD88, p-ASK1 NS and p-p38 in shHIF-1α transfected cells is significantly higher compared with the parental cells.

    TAK-242 purchased from MCE. Usage Cited in: Sci Rep. 2016 Jun 9;6:27866.

    Examination of TLR4 expression level in each group. The protein and mRNA levels of TLR4 are down-regulated by pretreatment with TAK-242.

    TAK-242 purchased from MCE. Usage Cited in: Sci Rep. 2016 Aug 4;6:30957.

    SEA promotes the senescence of LX-2 cells through activation of TLR4 signaling. Western blot analysis for P-p53 or TLR4 in LX-2 cells treated with SEA or TLR4 inhibitor TAK-242 (1 nM).

    TAK-242 purchased from MCE. Usage Cited in: Brain Behav Immun. 2017 Jan;59:322-332.

    Pretreatment with TAK-242 restores the reduction of hippocampal MBP induced by ds-HMGB1. (A and B) MBP content is detected by Western blot analysis using antibodies against MBP. GAPDH is used to control the load quantity.

    TAK-242 purchased from MCE. Usage Cited in: Am J Physiol Gastrointest Liver Physiol. 2016 Dec 1;311(6):G1091-G1104.

    Effects of TAK 242 and Catalpol on the expression of TLR-4 and activation of Src, PI3K, FAK, and Cathepsin B induced by LPS in HUVECs. Representative Western blots of TLR-4, p-Src, Src, p-PI3K, PI3K, p-FAK, FAK, activated cathepsin B, and cathepsin B proenzyme in different groups.

    TAK-242 purchased from MCE. Usage Cited in: Life Sci. 2017 Feb 1;170:25-32.

    Inhibition of TLR4 signaling attenuates PQ-induced NF-B activation and cytokine production. A549 cells are pre-treated 1 M TAK-242, followed by treatment with 300 M PQ for 24 h. The levels of (A) p-IB, (B) nuclear NF-B and (C) TLR4 are examined by Western blot analysis. (D) The relative mRNA expressions of TNF-, IL-1and IL-6 are measured by real-time PCR.

    TAK-242 purchased from MCE. Usage Cited in: Sci Rep. 2017 Mar 8;7:43834.

    Compared with the expression in the DM + MCAO group, the expression of Bcl-2, Bax, cleaved caspase-3, TNF-α, IL-1β and TLR4 proteins is greatly reduced in the DM + MCAO + TAK242 group.

    TAK-242 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Mar 29;41(4):1675-1683.

    TLR4 protein expression detected by western blot.

    TAK-242 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Mar 29;41(4):1675-1683.

    MyD88 protein expression detected by wes¬tern blot.

    TAK-242 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Mar 29;41(4):1675-1683.

    NF-κB p65 (nuclei) protein expression detec¬ted by western blot.

    TAK-242 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Mar 29;41(4):1675-1683.

    p-IκBα protein expression detected by wes¬tern blot.

    TAK-242 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Mar 29;41(4):1675-1683.

    Cleaved caspase-3 protein expression detec¬ted by western blot.

    TAK-242 purchased from MCE. Usage Cited in: Chin Med J (Engl). 2017 Apr 20;130(8):906-913.

    The levels of TLR4, IL-1β mRNA, and protein in TAK242 group are much lower than those in IgANTAK242 group.

    TAK-242 purchased from MCE. Usage Cited in: PLoS One. 2017 May 24;12(5):e0178147.

    (A) Titration of TAK-242 concentration. RPTC cells are cultured for 12 h in low glucose or high glucose medium with or without TAK-242. (B) MyD88 upregulation is also inhibited by TAK-242 under high glucose conditions by Western blotting.

    TAK-242 purchased from MCE. Usage Cited in: Oncotarget. 2017 May 9;8(19):31802-31814.

    Activation of the β-catenin signaling pathway by Fn (F01) can be inhibited by both the TLR4 inhibitor (TAK-242) and PAK1 inhibitor (IPA-3).

    TAK-242 purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3111-3116.

    TLR4 inhibitor TAK 242 suppresses the TLR4/IRAK/NF ΚB signaling pathway in PASMCs. Western blot analysis is performed to detect the levels of p IRAK, IRAK, p IKK, IKK, p IκB, IκB and NF κB p65, and the representative blot results are shown.

    TAK-242 purchased from MCE. Usage Cited in: Carbohydr Polym. 2018 Mar 1;183:207-218.

    TAK-242 significantly reduces the protein expression of p-JNK, p-ERK, p-p38, p-Akt and LC3-II.

    TAK-242 purchased from MCE. Usage Cited in: Sci Rep. 2018 Jan 24;8(1):1535.

    Effect of TAK242 on MAPKs phosphorylation in HUVECs treated with 9t18:1 and 11t18:1. HUVECs are treated with TAK242 (0.5, 1, 1.5 μM) for 30 min and then cultured with 9t18:1 for 24 h.

    TAK-242 purchased from MCE. Usage Cited in: Front Immunol. 2017 Dec 13;8:1808.

    The protein expression levels of Tgm2 in the 8-week Sj-infected mouse liver with TAK242 treatment are significantly reduced compared to those of the non-treated control.

    TAK-242 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jan 30;9:28.

    Effects of TAK-242 on the protein expressions of TLR4, MyD88, TRAF6, p-NF-κB p65, and total NF-κB p65 induced by Aβ1-42 in hBMECs by Western blotting analysis. The bands of TLR4, MyD88, TRAF6, p-NF-κB p65, total NF-κB p65, and β-actin. β-actin is used as a loading control.

    TAK-242 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 16 May 2018.

    HK-2 cells are treated with TLR4 inhibitor (TAK242, 5 μM) for 2 h prior to HG (30 mM) treatment for 2 h and with NF-κB blocker (Parthenolide, 10 μM) and HG (30 mM) for 2 h, and the samples are collected for Western blot analysis.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    TAK-242 is a potent TLR4 signaling inhibitor, selectively inhibits the TLR4-mediated production of cytokines and NO.

    IC50 & Target

    TLR4[1]

    In Vitro

    In RAW264.7 cells and mouse peritoneal macrophages, TAK-242 suppresses lipopolysaccharide (LPS)-induced production of NO, tumor necrosis factor-α (TNF-α), and interleukin (IL)-6, with IC50 of 1.1 to 11 nM. TAK-242 also suppresses the production of these cytokines from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM[1].

    In Vivo

    TAK-242 apparently reduces the serum anti-dsDNA levels in both genotype mice. Alternatively, IFN-γ, TNF-α, and IL-1β production is markedly inhibited by TAK-242, but their concentrations are still greatly higher than those in NS-treated counterparts[2]. TAK-242 pre-stress administration prevents the accumulation of potentially deleterious inflammatory and oxidative/nitrosative mediators in the brain frontal cortex of rats. TAK-242 i.v. administration at the beginning of the stress session completely blocks TLR-4 mRNA and protein upregulation after stress exposure[3].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.7638 mL 13.8190 mL 27.6381 mL
    5 mM 0.5528 mL 2.7638 mL 5.5276 mL
    10 mM 0.2764 mL 1.3819 mL 2.7638 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    TAK-242 is dissolved in N,N-dimethylformamide, and then diluted with appropriate medium before use[1].

    RAW264.7 cells are seeded at a density of 3×106 cells/well in six-well culture plate and incubated overnight. After washing with RPMI 1640 medium supplemented with 1% FCS and 10 μg/mL Kanamycin, the cells are stimulated with 5 ng/mL LPS and 1 U/mL IFN-γ in the presence or absence of TAK-242 (1-100 nM) for the indicated time. Culture supernatants are removed, and total RNA is isolated using the total RNA isolation reagent ISOGEN. Total RNA is reverse transcribed into cDNA by using TaqMan reverse transcription reagents. Quantitative real-time PCR analysis of TNF-α and IL-6 is performed on ABI Prism 7700 using predeveloped TaqMan assay reagents and Universal PCR master mix. Quantitation of mRNA is performed using the comparative threshold cycle method. The highest control level attained by the stimulation (without TAK-242) is regarded as 100%, and the levels of control group at other time points and TAK-242-added group are expressed as the percentage of the highest control level[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    TAK-242 is suspended in vehicle (saline) (Mice)[2].
    TAK-242 is suspended in vehicle (0.9% DMSO) (Rats)[3].

    Mice[2]
    Thirty ApoE-/- and thirty wild-type mice on C57BL/6 background (female, 10 weeks old) are fed on a high-fat diet containing 0.25% cholesterol and 15% cocoa butter under standardized lighting conditions (12 h light-dark cycle) and temperature (21±1°C). And mineral water is administered ad libitum. Mice of both genotypes are randomly assigned to LPS or LPS + TAK-242 or saline administration. LPS (2.5 mg/kg), LPS (2.5 mg/kg) plus TAK-242 (0.3 mg/kg) and saline are administered respectively by intraperitoneal injection, twice a week for 4 weeks. At the end of experiments, all mice underwent euthanasia with injection of overdose pentobarbital (50 mg/kg).
    Rats[3]
    Male outbred Wistar Hannover rats, initially weighing 200 to 225 g, are used. TAK-242 is i.v. injected in the tail vein at a dose of 0.5 mg/kg immediately after (approximately 10 seconds) introducing the animal to the plastic restrainer. This dose is chosen on the basis of previous in vivo studies reporting its anti-inflammatory/antioxidant and neuroprotective profile in microglia exposed to hypoxia. Dimethyl sulphoxide at a concentration of 0.9% is used as vehicle. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    361.82

    Formula

    C₁₅H₁₇ClFNO₄S

    CAS No.

    243984-11-4

    SMILES

    O=S([[email protected]]1C(C(OCC)=O)=CCCC1)(NC2=CC=C(C=C2Cl)F)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 360 mg/mL

    TAK-242 is dissolved in a fat emulsion (i.v. injection)[4].
    TAK-242 dissolved in DMSO (10 mg/mL) is diluted in DW[5].
    TAK-242 is prepared in 0.5% acetone[6].
    TAK-242 is prepare in vehicle (sterile saline)[7].
    TAK242 is prepared in PBS[8].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.95% ee.: 98.00%

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    Product Name:
    TAK-242
    Cat. No.:
    HY-11109
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