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

TAK-242 (Synonyms: Resatorvid)

Cat. No.: HY-11109 Purity: 99.95% ee.: 98.00%
Data Sheet SDS 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 $121 In-stock
5 mg $110 In-stock
10 mg $170 In-stock
50 mg $660 In-stock
100 mg $1100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • 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
NCT Number Sponsor Condition Start Date Phase
NCT00633477 Takeda Sepsis February 2008 Phase 3
NCT00143611 Takeda Sepsis September 2005 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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 dissolved in vehicle (saline) (Mice)[2].
TAK-242 is dissolved in vehicle (0.9% DMSO) (Rat)[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).
Rat[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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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].

* "<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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