Resatorvid, also known as TAK-242, is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules. Resatorvid provides neuroprotection in experimental traumatic brain injury: implication in the treatment of human brain injury.
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Name | Resatorvid |
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Iupac Chemical Name | ethyl (R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate |
Synonyms | TAK-242; TAK 242; TAK242; Resatorvid |
Molecular Formula | C15H17ClFNO4S |
Molecular Weight | 361.8124 |
Smile | FC1=CC(Cl)=C(NS([C@@H]2CCCC=C2C(OCC)=O)(=O)=O)C=C1 |
InChiKey | LEEIJTHMHDMWLJ-CQSZACIVSA-N |
InChi | InChI=1S/C15H17ClFNO4S/c1-2-22-15(19)11-5-3-4-6-14(11)23(20,21)18-13-8-7-10(17)9-12(13)16/h5,7-9,14,18H,2-4,6H2,1H3/t14-/m1/s1 |
CAS Number | 243984-11-4 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | Solid powder |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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Clinical study |
1: Feng Y, Gao J, Cui Y, Li M, Li R, Cui C, Cui J. Neuroprotective Effects of
Resatorvid Against Traumatic Brain Injury in Rat: Involvement of Neuronal
Autophagy and TLR4 Signaling Pathway. Cell Mol Neurobiol. 2016 Mar 10. [Epub
ahead of print] PubMed PMID: 26961544.
2: Zhang D, Li H, Li T, Zhou M, Hao S, Yan H, Yu Z, Li W, Li K, Hang C. TLR4
inhibitor resatorvid provides neuroprotection in experimental traumatic brain
injury: implication in the treatment of human brain injury. Neurochem Int. 2014
Sep;75:11-8. doi: 10.1016/j.neuint.2014.05.003. Epub 2014 May 20. PubMed PMID:
24858944.
3: Takeuchi T, Jinno F, Ebihara T, Moriya Y, Kadotani R, Tagawa Y, Kondo T, Itoh
T, Asahi S. 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. Biopharm Drug Dispos. 2013 May;34(4):236-46.
doi: 10.1002/bdd.1841. Epub 2013 May 7. PubMed PMID: 23529922.
4: Jinno F, Takeuchi T, Tagawa Y, Kondo T, Itoh T, Asahi S. Differences in the
pharmacokinetics of 4-amino-3-chlorophenyl hydrogen sulfate, a metabolite of
resatorvid, in rats and dogs. Drug Metab Dispos. 2012 Apr;40(4):648-54. doi:
10.1124/dmd.111.043729. Epub 2011 Dec 27. PubMed PMID: 22203697.
5: Matsunaga N, Tsuchimori N, Matsumoto T, Ii M. 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. Mol Pharmacol. 2011 Jan;79(1):34-41. doi: 10.1124/mol.110.068064. Epub
2010 Sep 29. PubMed PMID: 20881006.