RESATORVID
- CAS No.
- 243984-11-4
- Chemical Name:
- RESATORVID
- Synonyms
- CS-1150;TAK 242;Resatorvi;RESATORVID;TAK-242(Resatorvid);Resatorvid(TAK-242);RESATORVID; TAK242; TAK 242;(R)-ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate;Ethyl (R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]-1-cyclohexenecarboxylate;ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate
- CBNumber:
- CB92455670
- Molecular Formula:
- C15H17ClFNO4S
- Molecular Weight:
- 361.82
- MDL Number:
- MFCD11046362
- MOL File:
- 243984-11-4.mol
- MSDS File:
- SDS
| Melting point | 68-69℃ |
|---|---|
| Boiling point | 462.0±55.0 °C(Predicted) |
| Density | 1.39 |
| storage temp. | Sealed in dry,Room Temperature |
| solubility | insoluble in H2O; ≥100.6 mg/mL in EtOH; ≥18.09 mg/mL in DMSO |
| form | Solid |
| pka | 7.08±0.40(Predicted) |
| FDA UNII | H2MZ648C31 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| HS Code | 2935909099 | |||||||||
| NFPA 704 |
|
RESATORVID price More Price(51)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 614316 | TLR4 Inhibitor, TAK-242 - CAS 243984-11-4 - Calbiochem | 243984-11-4 | 5mg | $251 | 2024-03-01 | Buy |
| Sigma-Aldrich | 5.08336 | InSolution TLR4 Inhibitor, TAK-242 - CAS 243984-11-4 - Calbiochem | 243984-11-4 | 2mg | $126 | 2024-03-01 | Buy |
| Cayman Chemical | 13871 | TAK-242 ≥98% | 243984-11-4 | 1mg | $73 | 2024-03-01 | Buy |
| Cayman Chemical | 13871 | TAK-242 ≥98% | 243984-11-4 | 5mg | $217 | 2024-03-01 | Buy |
| Cayman Chemical | 13871 | TAK-242 ≥98% | 243984-11-4 | 10mg | $396 | 2024-03-01 | Buy |
RESATORVID Chemical Properties,Uses,Production
Uses
Resatorvid is a novel selective Toll-like receptor 4 signal transduction inhibitor. Resatorvid inhibits various kinds of inflammatory mediators such as nitric oxide (NO), tumor necrosis factor (TNF)-α, interleukin (IL)-1, IL-6, IL-10, macrophage inhibitory protein (MIP)-2 and prostaglandin E2 from lipopolysaccharide (LPS)-stimulated macrophages.
Uses
Resatorvid is a novel selective Toll-like receptor 4 signal transduction inhibitor. Resatorvid inhibits various kinds of inflammatory mediators such as nitric oxide (NO), tumor necrosis factor (TNF)-α , interleukin (IL)-1, IL-6, IL-10, macrophage inhibitory protein (MIP)-2 and prostaglandin E2 from lipopolysaccharide (LPS)-stimulated macrophages.
General Description
A cell-permeable cyclohexenecarboxylate that disrupts TLR4, but not TLR1-3 or TLR5-10, interaction with adaptor molecules TIRAP and TRAM via direct binding to TLR4 intracellular Cys747 residue.Shown to effectively inhibit TLR4-mediated cellular events (IC50 = 1.8, 1.3, and 1.9 nM, respectively, against LPS-induced NO, IL-6, and TNF-α production in murine RAW264.7 macrophages) in vitro and completely prevent LPS- (7 mg/kg, i.p.) induced death in mice (3 mg/kg; i.v.) in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 508336).
Biological Activity
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.
Biochem/physiol Actions
Cell permeable: yes
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].
IC 50
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].
storage
Store at -20°C
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.
[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.
RESATORVID Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 47465 | 58 |
| Zhengzhou Alfa Chemical Co.,Ltd | +8618530059196 | sale04@alfachem.cn | China | 12431 | 58 |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | info@finetechnology-ind.com | China | 9571 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9923 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| CR Corporation Lomited | fred.wen@crcorporation.cn | CHINA | 12069 | 58 |
View Lastest Price from RESATORVID manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2019-08-07 | RESATORVID
243984-11-4
|
US $3.00 / KG | 1KG | 99% | 100kg | Career Henan Chemical Co |
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- RESATORVID
243984-11-4
- US $3.00 / KG
- 99%
- Career Henan Chemical Co
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