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Resatorvid

Catalog No. TQ0181 CAS 243984-11-4

Synonyms: CLI-095, TAK-242

Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Resatorvid, CAS 243984-11-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 167.00
25 mg	In stock	$ 323.00
50 mg	In stock	$ 528.00
100 mg	In stock	$ 848.00
1 mL * 10 mM (in DMSO)	In stock	$ 118.00

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Purity: 100%

Purity: 99.73%

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Description	Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.
Targets&IC50	TNF R:1.9 nM , IL-6:1.3 nM , NO:1.8 nM
In vitro	METHODS: Breast cancer cell lines MCF7, SKBR3, MDA-MB-231 and BT-474 were treated with Resatorvid (10-150 µM) for 48 h. Cell viability was measured using MTT Assay. RESULTS: Resatorvid dose-dependently inhibited the viability of breast cancer cell lines. [1] METHODS: Macrophage RAW264.7 was treated with Resatorvid (1-100 nM) and LPS (5 ng/mL), IFN-γ (1 U/mL) for 4 h. Gene expression levels were measured by RT-qPCR. RESULTS: Resatorvid inhibited LPS and IFN-γ induced mRNA expression of IL-6 and TNF-α in RAW264.7 cells. [2]
In vivo	METHODS: To test the effects on cancer-comorbid depression (BCCD), Resatorvid (3 mg/kg) was administered intraperitoneally to BALB/c mice in the BCCD model once daily for three weeks. RESULTS: Resatorvid attenuated the symptoms of BCCD mice in vivo.Resatorvid inactivated inflammatory factors and TLR4/NF-κB/NLRP3 signaling pathway in vivo. [3] METHODS: To investigate the effects on temporomandibular joint osteoarthritis (TMJOA), Resatorvid (10 mg/kg) was injected intraperitoneally twice weekly for four weeks into a CFA-induced TMJOA model in C57BL/6 mice. RESULTS: Prophylactic treatment with Resatorvid attenuated TMJOA pathology by inhibiting chondrocyte focal prolapse and degeneration, and ROS-induced macrophage inflammation via TLR4/MyD88/NF-κB/NLRP3. [4]
Cell Research	Cell Line: RAW264.7 cells. Concentration: 1 nM, 10 nM, 100 nM. Incubation Time: 4 hours [1]
Animal Research	Animal Model: 30 ApoE knockout and 30 wild-type mice on a C57BL/6 background (female, 10 weeks old). Dosage: 0.3?mg/kg. Administration: i.p.; twice a week; for 4 weeks [3]

Synonyms	CLI-095, TAK-242
Molecular Weight	361.82
Formula	C15H17ClFNO4S
CAS No.	243984-11-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 100 mg/mL (276.38 mM), Sonication is recommended.

References and Literature

1. Zandi Z, et al. The anticancer effect of the TLR4 inhibition using TAK-242 (resatorvid) either as a single agent or in combination with chemotherapy: A novel therapeutic potential for breast cancer. J Cell Biochem. 2020 Feb;121(2):1623-1634. 2. Ii M, et al. A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling. Mol Pharmacol. 2006 Apr;69(4):1288-95. 3. Luo W, et al. Resatorvid Relieves Breast Cancer Complicated with Depression by Inactivating Hippocampal Microglia Through TLR4/NF-κB/NLRP3 Signaling Pathway. Cancer Manag Res. 2020 Dec 18;12:13003-13014. 4. Liu X, et al. Resatorvid alleviates experimental inflammatory TMJOA by restraining chondrocyte pyroptosis and synovial inflammation. Arthritis Res Ther. 2023 Nov 29;25(1):230.

Citations

1. Chen J, Zhao L, Ding X, et al. Aβ1–40 Oligomers Trigger Neutrophil Extracellular Trap Formation through TLR4- and NADPH Oxidase-Dependent Pathways in Age-Related Macular Degeneration. Oxidative Medicine and Cellular Longevity. 2022 2. Luo D, Han L, Gao S, et al. LINCS Dataset-Based Repositioning of Dutasteride as an Anti-Neuroinflammation Agent. Brain Sciences. 2021, 11(11): 1411.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Autophagy Compound Library NO PAINS Compound Library Bioactive Compound Library Bioactive Compounds Library Max Clinical Compound Library Immuno-Oncology Compound Library ReFRAME Related Library Apoptosis Compound Library

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Keywords

Resatorvid 243984-11-4 Apoptosis Autophagy Immunology/Inflammation TNF TLR Interleukin Inhibitor TAK 242 MyD88 inhibit TNF-R inflammatory diseases CLI-095 TNFR TAK-242 TRIF TNF Receptor CLI 095 CLI095 Tumor Necrosis Factor Receptor TAK242 Toll-like Receptor (TLR) Interleukin Related IL-6 inhibitor

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