Date published: 2025-12-11

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Resatorvid (CAS 243984-11-4)

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Alternate Names:
(6R)-6-[[(2-Chloro-4-fluorophenyl)amino]sulfonyl]-1-cyclohexene-1-carboxylic Acid Ethyl Ester; TAK 242
CAS Number:
243984-11-4
Molecular Weight:
361.82
Molecular Formula:
C15H17ClFNO4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Resatorvid is a novel synthetic compound developed by the pharmaceutical industry for laboratory experiments. Functioning as a selective agonist, it targets the G-protein-coupled receptor (GPCR) family, which plays a pivotal role in numerous physiological processes. It has been widely utilized in scientific research to explore the impact of GPCR activation on cellular physiology, including cell growth, differentiation, and programmed cell death. Moreover, its applications encompass the study of gene expression regulation and metabolic processes. By binding to GPCRs, Resatorvid acts as a selective agonist, initiating downstream signaling pathways upon receptor activation.


Resatorvid (CAS 243984-11-4) References

  1. TAK-242 (resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling, binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules.  |  Matsunaga, N., et al. 2011. Mol Pharmacol. 79: 34-41. PMID: 20881006
  2. Species differences of organic anion transporters involved in the renal uptake of 4-amino-3-chlorophenyl hydrogen sulfate, a metabolite of resatorvid, between rats and dogs.  |  Takeuchi, T., et al. 2013. Biopharm Drug Dispos. 34: 236-46. PMID: 23529922
  3. TLR4 inhibitor resatorvid provides neuroprotection in experimental traumatic brain injury: implication in the treatment of human brain injury.  |  Zhang, D., et al. 2014. Neurochem Int. 75: 11-8. PMID: 24858944
  4. Neuroprotective Effects of Resatorvid Against Traumatic Brain Injury in Rat: Involvement of Neuronal Autophagy and TLR4 Signaling Pathway.  |  Feng, Y., et al. 2017. Cell Mol Neurobiol. 37: 155-168. PMID: 26961544
  5. Pharmacological TLR4 Antagonism Using Topical Resatorvid Blocks Solar UV-Induced Skin Tumorigenesis in SKH-1 Mice.  |  Blohm-Mangone, K., et al. 2018. Cancer Prev Res (Phila). 11: 265-278. PMID: 29437671
  6. Berberine ameliorates diabetic nephropathy by inhibiting TLR4/NF-κB pathway.  |  Zhu, L., et al. 2018. Biol Res. 51: 9. PMID: 29604956
  7. 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.  |  Zandi, Z., et al. 2020. J Cell Biochem. 121: 1623-1634. PMID: 31535397
  8. Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation.  |  Plunk, MA., et al. 2020. ACS Med Chem Lett. 11: 141-146. PMID: 32071680
  9. Resatorvid Relieves Breast Cancer Complicated with Depression by Inactivating Hippocampal Microglia Through TLR4/NF-κB/NLRP3 Signaling Pathway.  |  Luo, W., et al. 2020. Cancer Manag Res. 12: 13003-13014. PMID: 33376394
  10. TLR4 pathway impairs synaptic number and cerebrovascular functions through astrocyte activation following traumatic brain injury.  |  Rosa, JM., et al. 2021. Br J Pharmacol. 178: 3395-3413. PMID: 33830504
  11. Harpagide alleviate neuronal apoptosis and blood-brain barrier leakage by inhibiting TLR4/MyD88/NF-κB signaling pathway in Angiotensin II-induced microglial activation in vitro.  |  Lu, Y., et al. 2021. Chem Biol Interact. 348: 109653. PMID: 34516974
  12. Design, Physicochemical Characterization, and In Vitro Permeation of Innovative Resatorvid Topical Formulations for Targeted Skin Drug Delivery.  |  Ruiz, VH., et al. 2022. Pharmaceutics. 14: PMID: 35456534
  13. Plerixafor and resatorvid inhibit hepatitis B virus in vitro by upregulating elongation factor Tu GTP-binding domain containing 2.  |  Cai, J., et al. 2023. Front Cell Infect Microbiol. 13: 1118801. PMID: 36891156

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Resatorvid, 5 mg

sc-476758
5 mg
$360.00