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

Resatorvid (Synonyms: TAK-242; CLI-095)

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

Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases. Resatorvid inhibits NO, TNF-R and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF.

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

Resatorvid Chemical Structure

Resatorvid Chemical Structure

CAS No. : 243984-11-4

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Customer Review

Based on 159 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE Resatorvid

    Resatorvid 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.

    Resatorvid 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.

    Resatorvid 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.

    Resatorvid 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).

    Resatorvid 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.

    Resatorvid 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.

    Resatorvid 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.

    Resatorvid purchased from MCE. Usage Cited in: Photochem Photobiol. 2016 Nov;92(6):816-825.

    Western blot analysis reveals that Resatorvid-based inhibition of TLR4 is able to block UV-induced phosphorylation of MAP kinases (p38 and JNK) and Akt.

    Resatorvid 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.

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

    TLR4 protein expression detected by western blot.

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

    MyD88 protein expression detected by western blot.

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

    NF-κB p65 (nuclei) protein expression detected by western blot.

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

    p-IκBα protein expression detected by western blot.

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

    Cleaved caspase-3 protein expression detected by western blot.

    Resatorvid 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.

    Resatorvid 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.

    Resatorvid 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).

    Resatorvid 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.

    Resatorvid purchased from MCE. Usage Cited in: Carbohyd 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.

    Resatorvid 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.

    Resatorvid 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.

    Resatorvid 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.

    Resatorvid purchased from MCE. Usage Cited in: Cancer Prev Res (Phila). 2018 May;11(5):265-278.

    There is a remarkable reduction in average levels of p21waf1 expression in the Prevention tumors compared to controls.

    Resatorvid purchased from MCE. Usage Cited in: Cell Immunol. 2018 Jun;328:86-92.

    Washed platelets are dealt with LPS (10 ug/mL, 30 min), LPS (10 ug/mL, 30 min) and TAK242 (132 nM, 30 min) or vehicle. PKC, AKT and p38 are detected by western blotting.

    Resatorvid purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2018 May 16;2018:6296802.

    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.

    Resatorvid purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;47(4):1497-1508.

    TAK-242 inhibits coronary microembolization (CME)-induced TLR4 upregulation and NLRP3 inflammasome activation.

    Resatorvid purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Aug;61:266-276.

    The protein expressions of TLR4 and NF-κB p65 are measured by western blot.

    Resatorvid purchased from MCE. Usage Cited in: Transplantation. 2018 Sep;102(9):1505-1513.

    Whole-islet lysates are prepared from islets with (TAK) or without (CTRL) early TLR4 blockade immediately after isolation (0 hours) and at 6- and 24-hours postisolation. Lysates are immunoblotted for ERK1/2, P38, SAPK, and P65, and analyzed for relative activation (phospho:total) normalized to β-actin.

    Resatorvid purchased from MCE. Usage Cited in: Front Immunol. 2018 Jul 23;9:1667.

    The inhibitory effect of TAK-242 on the TLR4 mRNA and protein expression is detected by RT-qPCR and Western Blot in NR8383 cells.

    Resatorvid purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Sep 4;15(1):252.

    The phosphorylation of NF-κB p65 evoked by Mrp14 is decreased after TAK-242 treatment.

    Resatorvid purchased from MCE. Usage Cited in: Cancer Sci. 2018 Aug;109(8):2391-2400.

    A549 cells pretreated with or without 5 μM TAK-242 and/or 10 μM PP1 (Src inhibitor) for 1 h are treated with 50 ng/mL Resistin for 15 min. Total protein is isolated and expression of phosphorylated (p-)Src, Src, p-EGFR, and EGFR is detected by Western blot

    Resatorvid purchased from MCE. Usage Cited in: Graefes Arch Clin Exp Ophthalmol. 2017 Nov;255(11):2199-2210.

    The effect of TAK-242 on the expression levels of NF-κB and MyD88 in retinal ganglion cells (RGCs) under high glucose are detected by Western blotting.

    Resatorvid purchased from MCE. Usage Cited in: Graefes Arch Clin Exp Ophthalmol. 2017 Nov;255(11):2199-2210.

    The effect of TAK-242 on the expression levels of TRAF6 and NLRP3 in retinal ganglion cells (RGCs) under high glucose are detected by Western blotting.

    Resatorvid purchased from MCE. Usage Cited in: PLoS One. 2015 Nov 10;10(11):e0142456.

    Renal protein expression of E-cadherin (an epithelial marker), and Fibronectin and a-SMA (mesenchymal markers) are assayed in rats treated with Aldo-salt or with Aldo-salt plus TAK-242. TAK-242 reverses the Aldo-salt-induced renal epithelial-mesenchymal transition.

    Resatorvid purchased from MCE. Usage Cited in: J Mol Neurosci. 2018 Dec;66(4):535-546.

    The increasing of TRAM1 is reversed by TAK242.

    Resatorvid purchased from MCE. Usage Cited in: J Mol Neurosci. 2018 Dec;66(4):535-546.

    In SC, p-NF-κB production is inhibited by TRAM1 siRNA or TAK242.

    Resatorvid purchased from MCE. Usage Cited in: J Mol Neurosci. 2018 Dec;66(4):535-546.

    In DRG, p-NF-κB production is inhibited by TRAM1 siRNA or TAK242.

    Resatorvid purchased from MCE. Usage Cited in: Neurosci Lett. 2018 Nov 1;686:33-40. 

    Western Blot analyses show the protein expression of MCPIP1 after the treatment of PBS and LPS (with TAK-242, C29, FPS-ZM1).

    Resatorvid purchased from MCE. Usage Cited in: Neurosci Lett. 2018 Nov 1;686:33-40. 

    Images show the expression of MCPIP1 after the treatment of of PBS and LPS (with TAK-242, C29, FPS-ZM1).

    Resatorvid purchased from MCE. Usage Cited in: EBioMedicine. 2018 Nov;37:78-90.

    TAK-242 alters NF-κB downstream targets in PSAP overexpressing SNB19 and GSC-21 cells as measured by western blotting.

    Resatorvid purchased from MCE. Usage Cited in: FASEB J. 2019 Mar;33(3):3451-3464.

    Western blot analyses of TLR4 and MAP4K4 in the retina of PN 17 OIR mice with or without TAK-242 and with or without ranibizumab treatment.

    Resatorvid purchased from MCE. Usage Cited in: FASEB J. 2019 Mar;33(3):3451-3464.

    Western blot analyses of TLR4 and MAP4K4, and moesin phosphorylation in HRMECs with the different treatments of TAK-242 or LPS.

    Resatorvid purchased from MCE. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. 

    Detection of PCNA by western blotting with the treatment of 2DG, MET and COM.

    Resatorvid purchased from MCE. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. 

    Detection of PCNA by immunohistochemistry with the treatment of 2DG, MET and COM.

    Resatorvid purchased from MCE. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. 

    The detection of cell cycle-related proteins by western blotting with the treatment of 2DG, MET and COM.

    Resatorvid purchased from MCE. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. 

    Detection of activated signaling molecules in the mTOR pathway via western blotting with the treatment of 2DG, MET and COM.

    Resatorvid purchased from MCE. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. 

    The detection of activated signaling molecules of the ERK pathway via western blotting with the treatment of 2DG, MET and COM.

    Resatorvid purchased from MCE. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. 

    Detection of the expression of key glucose metabolism enzymes via western blotting with the treatment of 2DG, MET and COM.

    Resatorvid purchased from MCE. Usage Cited in: Chem Biol Interact. 2019 Feb 1;299:179-185.

    Western blot analysis of TLR4 and MyD88 showing effect of TLR4 inhibitor (CLI-095) on PQ-induced inflammation in BV2 microglia. The blots are representative of three independent experiments. The bar diagrams which reflect mean fold change in the expression levels of TLR4 and MyD88 with respect to the control.

    Resatorvid purchased from MCE. Usage Cited in: Front Physiol. 2019 Mar 1;10:165.

    Effect of EP and TAK-242 treatment on CD68 protein expressions in aortic sinus of CUMS ApoE-/- mice. Over a 16-week period treatment, entire aorta from the aortic root to the iliac bifurcation is harvested, and then frozen-sections of aortic sinus are performed for immunofluorescent staining of CD68. Representative images of CD68 expression in aortic sinus.
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    Description

    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases. Resatorvid inhibits NO, TNF-R and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF[1][2].

    IC50 & Target

    TLR4

     

    In Vitro

    TAK-242 suppresses the production of NO, TNF-α, and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM[1].
    Resatorvid (1-100 nM; 4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells[1].
    Resatorvid (1-100 nM; 15 minutes; PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2), p38, and JNK/SAPK as well as degradation of IκBβ at a concentration of 100 nM[1].

    RT-PCR[1]

    Cell Line: RAW264.7 cells
    Concentration: 1 nM, 10 nM, 100 nM
    Incubation Time: 4 hours
    Result: TNF-α and IL-6 mRNA expression levels were clearly suppressed at concentrations of 10 to 100 nM.

    Western Blot Analysis[1]

    Cell Line: PBMCs cells
    Concentration: 1 nM, 10 nM, 100 nM
    Incubation Time: 15 minutes
    Result: The phosphorylation of mitogen-activated protein kinases induced by LPS was also inhibited in a concentration-dependent manner.
    In Vivo

    Resatorvid (0.3 mg/kg; intraperitoneal injection; twice a week; for 4 weeks; ApoE knockout and wild-type mice) treatment inhibites serum autoantibodies (ANA and anti-dsDNA), cytokines (IFN-γ, TNF-α, IL-1β), lung inflammation, and intima-media thickness in brachiocephalic artery[3].

    Animal Model: 30 ApoE knockout and 30 wild-type mice on C57BL/6 background (female, 10 weeks old)[3]
    Dosage: 0.3 mg/kg
    Administration: Intraperitoneal injection; twice a week; for 4 weeks
    Result: Inhibited serum autoantibodies (ANA and anti-dsDNA), cytokines (IFN-γ, TNF-α, IL-1β), lung inflammation, and intima-media thickness in brachiocephalic artery.
    Clinical Trial
    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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (276.38 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.75 mg/mL (7.60 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.75 mg/mL (7.60 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.75 mg/mL (7.60 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Product Name:
    Resatorvid
    Cat. No.:
    HY-11109
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