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| TAK-242TLR 4 signaling inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.50%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
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| Kinase experiment [1]: | |
Assay for LPS binding to PBMCs | PBMCs were suspended in BSA solution (phosphate-buffered saline containing 0.1% BSA and 0.01% sodium azide). In a total volume of 50 μL, PBMCs (3 × 105 cells) were incubated with TAK-242, anti-human CD14 monoclonal antibody (MAb) MEM-18, or anti-human CC-chemokine receptor 5 (CCR5) MAb as a negative control for 30 mins at 4 °C. The cells were further incubated with 50 ng/mL LPS from E. coli serotype O55:B5 conjugated with Alexa Fluor 488 per milliliter in the presence of human serum at a final concentration of 1% for 45 mins at 37 °C. After washing twice with BSA solution, 1 × 104 cells were analyzed by flow cytometry using CytoACE300 cytofluorometer. The assays were performed in triplicate for each preparation of PBMCs obtained from four different donors. Specific LPS binding was estimated by subtracting the percentage of LPS-binding cells in the absence of LPS from that in the presence of LPS. |
| Cell experiment [2]: | |
Cell lines | RAW264.7 cells |
Preparation method | This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 1, 10, 100 and 1000 nM; 15 mins |
Applications | In RAW264.7 cells, TAK-242 inhibited the phosphorylation of IRAK-1 induced by LPS. |
| Animal experiment [3]: | |
Animal models | Wistar Hannover rats |
Dosage form | 0.5 mg/kg; i.v. |
Applications | TAK-242 prevented the accumulation of potentially deleterious inflammatory and oxidative/nitrosative mediators in the brain frontal cortex of rats. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Ii M, Matsunaga N, Hazeki K, Nakamura K, Takashima K, Seya T, Hazeki O, Kitazaki T, Iizawa Y. 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;69(4):1288-95. [2]. Naoko Matsunaga, Noboru Tsuchimori, Tatsumi Matsumoto, and Masayuki Ii. 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 79:34–41, 2011. [3] Iciar Gárate, Borja García-Bueno, José Luis Mu?oz Madrigal, Javier R Caso, Luis Alou, María Luisa Gómez-Lus and Juan Carlos Leza. Toll-like 4 receptor inhibitor TAK-242 decreases neuroinflammation in rat brain frontal cortex after stress. Journal of Neuroinflammation 2014, 11:8. | |
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| Cas No. | 243984-11-4 | SDF | Download SDF |
| Synonyms | Resatorvid;TAK242;TAK 242;CLI-095 | ||
| Chemical Name | ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate | ||
| Canonical SMILES | CCOC(=O)C1=CCCCC1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl | ||
| Formula | C15H17ClFNO4S | M.Wt | 361.82 |
| Solubility | ≥18.091 mg/mL in DMSO, ≥100.6 mg/mL in EtOH, <2.45 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: With IC50 of 1.1 to 11 nM, TAK-242 inhibited LPS-induced NO production, tumor necrosis factor-alpha and interleukin (IL)-6 in RAW264.7 cells and mouse peritoneal macrophages [1].
Toll, a member of the Toll-like receptor (TLR) family, was identified as a gene product essential for the development of embryonic dorsoventral polarity in Drosophila melanogaster. Moreover, it has been also found to play a critical role in the antifungal response of flies. TAK-242 (resatorvid), a cyclohexene derivative, is recongnizred as a novel small-molecule compound selectively inhibiting TLR4 signaling.
In vitro: A previous in-vitro study showed that TAK-242 could inhibit the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4 using coimmunoprecipitation approach. Among 10 different human TLRs, TAK-242 selectively bound to TLR4. These findings suggested that TAK-242 could selectively bind to TLR4 and disrupted the interaction of TLR4 with adaptor molecules, thereby inhibiting TLR4 signal transduction and its downstream signaling [2].
In vivo: Preclinical animal study demonostrated that the acute restraint stress exposure upregulateed TLR-4 expression both at the mRNA and protein level in rat. TAK-242 pre-stress administration prevented the accumulation of potentially deleterious inflammatory and oxidative/nitrosative mediators in the brain frontal cortex of rats. These finding s indicated that the use of TAK-242 or other TLR-4 signalling pathway inhibitory compounds could be considered as a potential therapeutic adjuvant strategy to constrain the inflammatory process taking place after stress exposure and in stress-related neuropsychiatric diseases [3].
Clinical trial: To evaluate whether TAK-242, a small-molecule inhibitor of Toll-like receptor-4–mediated signaling, suppresses cytokine levels and improves 28-day all-cause mortality rates in patients with severe sepsis has been conducted in Japan, the U.S. and Europe by Takeda Pharmaceutical Company Limited ("Takeda"). However, following a thorough review of development strategy, Takeda has concluded that TAK-242’s profile does not meet the criteria to support continuation of further development activities. This decision has not been influenced by any concerns over the safety or efficacy of the compound [4].
Reference:[1] Ii M, Matsunaga N, Hazeki K, Nakamura K, Takashima K, Seya T, Hazeki O, Kitazaki T, Iizawa Y. 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;69(4):1288-95. [2] Naoko Matsunaga, Noboru Tsuchimori, Tatsumi Matsumoto, and Masayuki Ii. 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 79:34–41, 2011. [3] Iciar Gárate, Borja García-Bueno, José Luis Mu oz Madrigal, Javier R Caso, Luis Alou, María Luisa Gómez-Lus and Juan Carlos Leza. Toll-like 4 receptor inhibitor TAK-242 decreases neuroinflammation in rat brain frontal cortex after stress. Journal of Neuroinflammation 2014, 11:8.[4] Todd W. Rice; Arthur P. Wheeler; Gordon R. Bernard; Jean-Louis Vincent; Derek C. Angus; Naoki Aikawa; Ignace Demeyer; Stephen Sainati; Nicholas Amlot; Charlie Cao; Masayuki Ii; Hideyasu Matsuda; Kouji Mouri; Jon Cohen. A randomized, double-blind, placebo-controlled trial of TAK-242 for the treatment of severe sepsis. Crit Care Med 2010 Vol. 38, No. 8: 1-10.
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实验需要请问有没有养THP-1细胞的同仁？能否寄一皿我，我在广州南方医科大学，不胜感激！
激光共聚焦的看活细胞皿哪里买呢
想问下各位大神，本人用皿养的PC-9GR细胞突然有大片飘起，也并没有成团状飘起，求解决方法？
如题~
已经基本养好了贴壁的原代细胞了，准备鉴定了，看到好多都在说细胞爬片的问题，我可以不做爬片直接在皿里操作吗？具体需要注意些什么呢？感谢各位大神
ps：大皿和6孔板里细胞密度、培养条件等等都几乎一样。
我看园子里有人提过类似的问题，但还没人给出答案，希望有经验或有想法的战友帮忙分析分析啊~谢谢！
同学说传代必须是一皿传多皿，一皿传一皿就不算传代~求高手指点~~
传代后5天，依然没有长满，怕影响活力，想传代和冻存，不知这样是否可以？？
做细胞实验快半年了，一直都还挺顺的，这次五一放完假回来，复苏一支HK2，操作都跟以前一样，没想到出了好多问题：
冻存方法：包裹棉花直接-80℃过夜，第二天转移到液氮
冻存时间：1个半月前冻存的细胞，密度保证没问题，冻存前状态也好
复苏方法：液氮取出后37℃水浴，约2分钟溶解，加入6倍体积的完全培养基，800转离心5分钟，弃去上清，1ml完全培养基重悬，转移入培养皿（进口一次性塑料培养大皿），补足完全培养基，培养箱培养
第二天看细胞全都没贴壁，但是也没死，聚集成团装飘着，没有污染。不想重新离心加重机械损伤，就一直试试看的心态放在培养箱里养着了。又重新复苏一支，还是一样的结果，全飘着没贴壁。不死心，就往前面复苏的那一皿里直接加了1ml的血清，相当于18%的血清比例，过了一天去看，这下细胞都贴壁了。没有另外添加血清的那一皿就还是没贴壁。
另外还有一支以前复苏的HK2，也是一样的方法复苏的，那次复苏很好，细胞基本没什么死的，也都贴壁了，养在皿里状态也不错，但是拿来铺板就还是不贴壁，同样的培基（10%血清），铺板就一个不贴，皿里就都可以贴上。
求助各位战友：
1、复苏不贴壁是为什么？
2、增加血清比例能使复苏的细胞贴壁，这样的细胞是不是可以认为状态并不好，以后的培养是不是要一直这么高比例的血清？还是可以培养一段时间逐步减少血清比例？
3、仍然是10%血清，为什么铺板就不贴壁，而皿里的就没事？是不是铺板的时候也要增加血清比例呢？那在板里干预的过程中是不是要一直保持高比例的血清培养？
4、我的冻存及复苏方法是否有错？我觉得我的HK2从形态、生长速度上来说状态应该是不错的，而且我已经更换了全新的培基、血清和双抗，重新配置了完全培养基，不知道为什么会出现这种不贴壁的问题
拜托各位集思广益，细胞实验已经为了这个不贴壁的问题停滞快2周，心急如焚啊，拜托各位！
