Resatorvid (TAK-242)

Catalog No.S7455 Synonyms: CLI-095

For research use only.

Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.

Resatorvid (TAK-242) Chemical Structure

CAS No. 243984-11-4

Selleck's Resatorvid (TAK-242) has been cited by 21 publications

Purity & Quality Control

Choose Selective TLR Inhibitors

Biological Activity

Description Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
Targets
TLR4 [1] IL-6 [5]
(Cell-free assay)
NO [5]
(Cell-free assay)
TNF-α [5]
(Cell-free assay)
1.3 nM 1.8 nM 1.9 nM
In vitro

TAK-242 inhibits the TLR4 pathway by binding directly to a Cys747 in the intracellular TLR4 domain. TAK-242 disrupts the interactions of TLR4 with its adaptor molecules, TIRAP and TRAM[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RAW264.7 M365NGZ2dmO2aX;uJIF{e2G7 M1X1OGlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgTWw3KHC{b3T1Z5Rqd25iaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[nliRVzJV2EtKEmFNUCgQUAxNjByMUOg{txONg>? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjJ5OUiwOUc,OTZ{N{m4NFU9N2F-
RAW264.7 NWDTPZJCTnWwY4Tpc44h[XO|YYm= NXW5e|BDUW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBvcXS{aXOgc5hq\GVicILv[JVkfGmxbjDpckBud3W|ZTDSRXczPjRwNzDj[YxteyxiSVO1NEA:KDBwMECxPEDPxE1w MnvxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ{N{m4NFUoRjF4Mke5PFA2RC:jPh?=
RAW264.7 M3TabGZ2dmO2aX;uJIF{e2G7 NF7zTnNKdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJHRPTmGucHjhJJBzd2S3Y4Tpc44hcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZpkhTUyLU1GsJGlEPTBiPTCwMlAxOTlizszNMi=> M3LQdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4Mke5PFA2Lz5zNkK3PVgxPTxxYU6=
HEK-Blue MmL1SpVv[3Srb36gZZN{[Xl? NFTYbFczKGi{cx?= Mk[xTY5pcWKrdHnvckBw\iCqdX3hckBVVFJ2IIPp[45idGmwZzDlfJBz\XO|ZXSgbY4hUEWNLVLseYUh[2WubIOgZ48u\XiycnXzd4lv\yCPREKvR2QyPCCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hVFCVLXnu[JVk\WRiTl[tb4FxeGGEIHHjeIl3[XSrb36tcYVlcWG2ZXSgV2VCWCCycn;keYN1cW:wIIDy[Ylv[3WkYYTl[EBnd3JiMjDodpMh\m:ubH;3[YQh[nliTGDTJJN1cW23bHH0bY9vKG[xcjCyNEBpenNiYomgZ49td3KrbXX0dolkKGG|c3H5MEBKSzVyIE2gNE43QCEQvF2u NFf0dXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS3NlEzPid-Mkm0O|IyOjZ:L3G+
Assay
Methods Test Index PMID
Western blot TLR4 / p-p65 / p65 / pIκBα / IκBα ; Bcl-2 / Cleaved caspase-3 29207635
Immunofluorescence TLR4 ; NFκB 29311802
In vivo

TAK-242 protects against acute cerebral ischemia/reperfusion injury in mice by dose of 3 mg/kg[1]. Topical resatorvid can block UV-induced AP-1 activation in mouse epidermis. In a UV-induced skin tumorigenesis model, topical resatorvid displays potent photochemopreventive activity, significantly suppressing tumor area and multiplicity. Tumors harvested from resatorvid-treated mice display reduced activity of UV-associated signaling pathways and a corresponding increase in apoptosis compared to tumors from control animals[2]. TAK-242 significantly reduces the neuronal damage occurring after cerebral ischemia, a form of stroke in mice[3].

Protocol (from reference)

Cell Research:

[4]

  • Cell lines: Primary human keratinocytes
  • Concentrations: 10 µM
  • Incubation Time: 6 h
  • Method:

    NF-κB keratinocytes are treated with UVB +/− 10 µM resatorvid (or vehicle) and harvested 6 hr later. Resatorvid significantly inhibits UV-induced NF-κB luciferase signaling in keratinocytes.

Animal Research:

[3]

  • Animal Models: male ddY mice aged 4-5weeks
  • Dosages: 1 μl (at 0.001, 0.03, or 0.01 μg/μl)
  • Administration: intracerebroventricularly

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 361.82
Formula

C15H17ClFNO4S

CAS No. 243984-11-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C1=CCCCC1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04620148 Not yet recruiting Drug: TAK-242|Drug: Placebo Acute-On-Chronic Liver Failure Akaza Bioscience Ltd|Iqvia Pty Ltd December 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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