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MedKoo Cat#: 326750 | Name: Resatorvid
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Resatorvid, also known as TAK-242, is a cell-permeable inhibitor of TLR4 signaling. It binds directly to cysteine residue 747 intracellularly, preventing TLR4 binding with TIRAP and thus preventing downstream signal transduction. TAK-242 inhibits glioblastoma invasion, migration, and proneural-mesenchymal transition by inhibiting TLR4 signaling. AK-242 improves sepsis-associated acute kidney injury in rats by inhibiting the TLR4/NF-κB signaling pathway.

Chemical Structure

Resatorvid
Resatorvid
CAS#243984-11-4

Theoretical Analysis

MedKoo Cat#: 326750

Name: Resatorvid

CAS#: 243984-11-4

Chemical Formula: C15H17ClFNO4S

Exact Mass: 361.0551

Molecular Weight: 361.81

Elemental Analysis: C, 49.80; H, 4.74; Cl, 9.80; F, 5.25; N, 3.87; O, 17.69; S, 8.86

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 550.00 2 Weeks
50mg USD 950.00 2 Weeks
100mg USD 1,650.00 2 Weeks
1g USD 5,850.00 2 Weeks
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Related CAS #
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Synonym
TAK-242; TAK 242; TAK242; Resatorvid
IUPAC/Chemical Name
ethyl (R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate
InChi Key
LEEIJTHMHDMWLJ-CQSZACIVSA-N
InChi Code
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
SMILES Code
FC1=CC(Cl)=C(NS([C@@H]2CCCC=C2C(OCC)=O)(=O)=O)C=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
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
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s 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, plays pivotal role in various inflammatory diseases, and provides neuroprotection in experimental traumatic brain injury treatment.
In vitro activity:
This study identified resatorvid as a novel hepatitis B virus inhibitor in vitro. These findings provide information on the development of a new class of anti-hepatitis B virus agents that act on host factors rather than viral enzymes. Reference: Front Cell Infect Microbiol. 2023 Feb 20;13:1118801. https://pubmed.ncbi.nlm.nih.gov/36891156/
In vivo activity:
Resatorvid appears to exert a neuroprotective effect after HIBD by inhibiting activation of autophagy and the release of inflammatory cytokines via inhibition of the TLR4/NF-κB signaling pathway. Reference: Neural Regen Res. 2020 Jul;15(7):1316-1325. https://pubmed.ncbi.nlm.nih.gov/31960818/
Solvent mg/mL mM
Solubility
DMSO 100.0 276.38
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 361.81 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Cai J, Li Y, Hu P, Xu R, Yuan H, Zhang W, Feng T, Liu R, Li W, Zhu C. Plerixafor and resatorvid inhibit hepatitis B virus in vitro by upregulating elongation factor Tu GTP-binding domain containing 2. Front Cell Infect Microbiol. 2023 Feb 20;13:1118801. doi: 10.3389/fcimb.2023.1118801. PMID: 36891156; PMCID: PMC9986551. 2. Kashani B, Zandi Z, Bashash D, Zaghal A, Momeny M, Poursani EM, Pourbagheri-Sigaroodi A, Mousavi SA, Ghaffari SH. Small molecule inhibitor of TLR4 inhibits ovarian cancer cell proliferation: new insight into the anticancer effect of TAK-242 (Resatorvid). Cancer Chemother Pharmacol. 2020 Jan;85(1):47-59. doi: 10.1007/s00280-019-03988-y. Epub 2019 Nov 30. PMID: 31786654. 3. Jiang LJ, Xu ZX, Wu MF, Dong GQ, Zhang LL, Gao JY, Feng CX, Feng X. Resatorvid protects against hypoxic-ischemic brain damage in neonatal rats. Neural Regen Res. 2020 Jul;15(7):1316-1325. doi: 10.4103/1673-5374.272615. PMID: 31960818; PMCID: PMC7047798. 4. Blohm-Mangone K, Burkett NB, Tahsin S, Myrdal PB, Aodah A, Ho B, Janda J, McComas M, Saboda K, Roe DJ, Dong Z, Bode AM, Petricoin EF 3rd, Calvert VS, Curiel-Lewandrowski C, Alberts DS, Wondrak GT, Dickinson SE. Pharmacological TLR4 Antagonism Using Topical Resatorvid Blocks Solar UV-Induced Skin Tumorigenesis in SKH-1 Mice. Cancer Prev Res (Phila). 2018 May;11(5):265-278. doi: 10.1158/1940-6207.CAPR-17-0349. Epub 2018 Feb 1. PMID: 29437671; PMCID: PMC5932085.
In vitro protocol:
1. Cai J, Li Y, Hu P, Xu R, Yuan H, Zhang W, Feng T, Liu R, Li W, Zhu C. Plerixafor and resatorvid inhibit hepatitis B virus in vitro by upregulating elongation factor Tu GTP-binding domain containing 2. Front Cell Infect Microbiol. 2023 Feb 20;13:1118801. doi: 10.3389/fcimb.2023.1118801. PMID: 36891156; PMCID: PMC9986551. 2. Kashani B, Zandi Z, Bashash D, Zaghal A, Momeny M, Poursani EM, Pourbagheri-Sigaroodi A, Mousavi SA, Ghaffari SH. Small molecule inhibitor of TLR4 inhibits ovarian cancer cell proliferation: new insight into the anticancer effect of TAK-242 (Resatorvid). Cancer Chemother Pharmacol. 2020 Jan;85(1):47-59. doi: 10.1007/s00280-019-03988-y. Epub 2019 Nov 30. PMID: 31786654.
In vivo protocol:
1. Jiang LJ, Xu ZX, Wu MF, Dong GQ, Zhang LL, Gao JY, Feng CX, Feng X. Resatorvid protects against hypoxic-ischemic brain damage in neonatal rats. Neural Regen Res. 2020 Jul;15(7):1316-1325. doi: 10.4103/1673-5374.272615. PMID: 31960818; PMCID: PMC7047798. 2. Blohm-Mangone K, Burkett NB, Tahsin S, Myrdal PB, Aodah A, Ho B, Janda J, McComas M, Saboda K, Roe DJ, Dong Z, Bode AM, Petricoin EF 3rd, Calvert VS, Curiel-Lewandrowski C, Alberts DS, Wondrak GT, Dickinson SE. Pharmacological TLR4 Antagonism Using Topical Resatorvid Blocks Solar UV-Induced Skin Tumorigenesis in SKH-1 Mice. Cancer Prev Res (Phila). 2018 May;11(5):265-278. doi: 10.1158/1940-6207.CAPR-17-0349. Epub 2018 Feb 1. PMID: 29437671; PMCID: PMC5932085.
1: Yang T, Li Y, Su B. 循环组蛋白诱导内皮功能障碍致脓毒症急性呼吸窘迫综合征的机制研究 [Mechanism of Extracellular Histone-Induced Endothelial Dysfunction Leading to Sepsis-Induced Acute Respiratory Distress Syndrome]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2024 Jul 20;55(4):902-910. Chinese. doi: 10.12182/20240760508. PMID: 39170019; PMCID: PMC11334276. 2: Dik B, Hatipoglu D, Ates MB. Potential effects of Resatorvid and alpha lipoic acid on gentamicin-induced nephrotoxicity in rats. Pharmacol Res Perspect. 2024 Aug;12(4):e1222. doi: 10.1002/prp2.1222. PMID: 38992963; PMCID: PMC11239954. 3: Asurappulige HSH, Ladomery MR, Ruth Morse H. IL-6 knockdown in a model of the human bone marrow, abrogates DNA damage induction in bystander cells post- chemotherapy induced cytokine release syndrome. Transl Oncol. 2024 Aug;46:102030. doi: 10.1016/j.tranon.2024.102030. Epub 2024 Jun 12. PMID: 38870677; PMCID: PMC11222933. 4: Khomeijani-Farahani M, Karami J, Farhadi E, Soltani S, Delbandi AA, Shekarabi M, Tahmasebi MN, Vaziri AS, Jamshidi A, Mahmoudi M, Akhlaghi M. TAK-242 (Resatorvid) inhibits proinflammatory cytokine production through the inhibition of NF-κB signaling pathway in fibroblast-like synoviocytes in osteoarthritis patients. Adv Rheumatol. 2024 Jun 7;64(1):46. doi: 10.1186/s42358-024-00385-9. PMID: 38849923. 5: Huang X, Lin R, Liu H, Dai M, Guo J, Hui W, Liu W, Haerken M, Zheng R, Yushanjiang T, Gao F. Resatorvid (TAK-242) Ameliorates Ulcerative Colitis by Modulating Macrophage Polarization and T Helper Cell Balance via TLR4/JAK2/STAT3 Signaling Pathway. Inflammation. 2024 May 18. doi: 10.1007/s10753-024-02028-z. Epub ahead of print. PMID: 38760646. 6: Feng Z, Chen G, Huang Y, Zhang K, Wu G, Xing W, Wu Y, Zhou Y, Sun C. TAK-242 inhibits glioblastoma invasion, migration, and proneural-mesenchymal transition by inhibiting TLR4 signaling. Exp Cell Res. 2024 Jun 1;439(1):114091. doi: 10.1016/j.yexcr.2024.114091. Epub 2024 May 11. PMID: 38740168. 7: Wang J, Li H, Liu Y, Andrzejczyk NE, Qiao K, Ma Y, Zhou S, Gui W, Zhu G, Li S, Schlenk D. Contribution of Immune Responses to the Cardiotoxicity and Hepatotoxicity of Deltamethrin in Early Life Stage Zebrafish (Danio rerio). Environ Sci Technol. 2024 Jun 4;58(22):9515-9524. doi: 10.1021/acs.est.3c10682. Epub 2024 Apr 30. PMID: 38687472. 8: Oh H, Makita Y, Masuno K, Imamura Y. Hangeshashinto Inhibits Porphyromonas gingivalis Pathogen-Associated Molecular Patterns-Mediated IL-6 and IL-8 Production through Toll-Like Receptors in CAL27 Cells. Evid Based Complement Alternat Med. 2024 Apr 18;2024:9866670. doi: 10.1155/2024/9866670. PMID: 38665937; PMCID: PMC11045287. 9: Bian B, Miao X, Zhao X, Lai C, Chen Y, Zhou M, Yong Q. Impacts of monosaccharide composition on immunomodulation by cello-pentaose, manno- pentaose, and xylo-pentaose: Unraveling the underlying molecular mechanisms. Carbohydr Polym. 2024 Jun 15;334:122006. doi: 10.1016/j.carbpol.2024.122006. Epub 2024 Feb 29. PMID: 38553211. 10: Du R, Chen S, Han C, He Z, Pei H, Yang Y. M1 intestinal macrophages-derived exosomes promote colitis progression and mucosal barrier injury. Aging (Albany NY). 2024 Mar 26;16(6):5703-5710. doi: 10.18632/aging.205672. Epub 2024 Mar 26. PMID: 38535999; PMCID: PMC11006457. 11: Cho DE, Hong JP, Kim Y, Sim JY, Kim HS, Kim SR, Lee B, Cho HS, Cho IH, Shin S, Yeom M, Kwon SK, Lee IS, Park H, Kim K, Hahm DH. Role of gut-derived bacterial lipopolysaccharide and peripheral TLR4 in immobilization stress- induced itch aggravation in a mouse model of atopic dermatitis. Sci Rep. 2024 Mar 15;14(1):6263. doi: 10.1038/s41598-024-56936-z. PMID: 38491103; PMCID: PMC10942979. 12: Mao Y, Yu J, Yuan J, DA J, Yu F, Zha Y. [High mobility group nucleosome binding protein 1 (HMGN1) induces activation of mouse BV2 microglia and upregulates their pro-inflammatory mediator expression by activating TLR4/MyD88/NF-κB p65/IKK-β signal pathway]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2024 Feb;40(2):135-141. Chinese. PMID: 38284254. 13: Cao Y, Yao W, Lu R, Zhao H, Wei W, Lei X, Zhang Z, Liu B. Reveal the correlation between hub hypoxia/immune-related genes and immunity and diagnosis, and the effect of SAP30 on cell apoptosis, ROS and MDA production in cerebral ischemic stroke. Aging (Albany NY). 2023 Dec 27;15(24):15161-15182. doi: 10.18632/aging.205339. Epub 2023 Dec 27. PMID: 38154101; PMCID: PMC10781503. 14: Wu Y, Zhang Y, Tang X, Ye S, Shao J, Tu L, Pan J, Chen L, Liang G, Yin L. Synergistic anti-oxidant and anti-inflammatory effects of ceria/resatorvid co- decorated nanoparticles for acute lung injury therapy. J Nanobiotechnology. 2023 Dec 21;21(1):502. doi: 10.1186/s12951-023-02237-y. PMID: 38129906; PMCID: PMC10740228. 15: Liu X, Li H, Feng Y, Guo H, Li Y, Ke J, Long X. Resatorvid alleviates experimental inflammatory TMJOA by restraining chondrocyte pyroptosis and synovial inflammation. Arthritis Res Ther. 2023 Nov 29;25(1):230. doi: 10.1186/s13075-023-03214-4. PMID: 38031141; PMCID: PMC10685467. 16: Xie J, Tuo P, Zhang W, Wang S. Inhibition of the TLR4/NF-κB pathway promotes the polarization of LPS-induced BV2 microglia toward the M2 phenotype. Neuroreport. 2023 Dec 6;34(17):834-844. doi: 10.1097/WNR.0000000000001961. Epub 2023 Oct 18. PMID: 37938926. 17: Lin Z, Ru L, Wang H, Mao K. TLR4 Inhibition Protects against Retinal Ganglion Cell Damage in Rats with Chronic Ocular Hypertension. Discov Med. 2023 Oct;35(178):796-804. doi: 10.24976/Discov.Med.202335178.74. PMID: 37811617. 18: Fu H, Zhang P, Zhao XD, Zhong XY. Interfering with Rac1-activation during neonatal monocyte-macrophage differentiation influences the inflammatory responses of M1 macrophages. Cell Death Dis. 2023 Sep 21;14(9):619. doi: 10.1038/s41419-023-06150-y. PMID: 37735499; PMCID: PMC10514032. 19: Granata S, Bruschi M, Verlato A, Pontrelli P, Gesualdo L, Stallone G, Zaza G. Autophagy Activation in Peripheral Blood Mononuclear Cells of Peritoneal Dialysis Patients. Kidney Int Rep. 2023 Jun 26;8(9):1852-1863. doi: 10.1016/j.ekir.2023.06.017. PMID: 37705917; PMCID: PMC10496084. 20: Feng Y, Ju Y, Wu Q, Sun G, Yan Z. TAK-242, a toll-like receptor 4 antagonist, against brain injury by alleviates autophagy and inflammation in rats. Open Life Sci. 2023 Jul 29;18(1):20220662. doi: 10.1515/biol-2022-0662. PMID: 37528888; PMCID: PMC10389675.