RESATORVID
- Product Name
- 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
- Formula Weight
- 361.82
- MOL File
- 243984-11-4.mol
RESATORVID Property
- 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)
- color
- Off-white to yellow
Safety
- HS Code
- 2935909099
N-Bromosuccinimide Price
- Product number
- 614316
- Product name
- TLR4 Inhibitor, TAK-242 - CAS 243984-11-4 - Calbiochem
- Packaging
- 5mg
- Price
- $251
- Updated
- 2024/03/01
- Product number
- 5.08336
- Product name
- InSolution TLR4 Inhibitor, TAK-242 - CAS 243984-11-4 - Calbiochem
- Packaging
- 2mg
- Price
- $126
- Updated
- 2024/03/01
- Product number
- 13871
- Product name
- TAK-242
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 13871
- Product name
- TAK-242
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $217
- Updated
- 2024/03/01
- Product number
- 13871
- Product name
- TAK-242
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $396
- Updated
- 2024/03/01
RESATORVID Chemical Properties,Usage,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.
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
RESATORVID Suppliers
- Tel
- +86-21-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6005
- Advantage
- 61
- Tel
- 13611719524
- 2674347328@qq.com
- Country
- China
- ProdList
- 53
- Advantage
- 58
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- 010-82848833 400-666-7788
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 94657
- Advantage
- 76
- Tel
- 021-50135380
- shchemsky@sina.com
- Country
- China
- ProdList
- 15402
- Advantage
- 60
- Tel
- 0411-62910999 13889544652
- meilunui@163.com
- Country
- China
- ProdList
- 4727
- Advantage
- 58
- Tel
- +86057186818502 13588463833
- Fax
- Pls mail us for more information!
- info@sagechem.com
- Country
- China
- ProdList
- 10266
- Advantage
- 58
- Tel
- 010-56205725
- Fax
- 010-65763397
- waley188@sohu.com
- Country
- China
- ProdList
- 12335
- Advantage
- 58
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
- Tel
- 400-400-6206333 18521732826
- Fax
- 021-50323701
- market@aladdin-e.com
- Country
- China
- ProdList
- 25003
- Advantage
- 65
- Tel
- 021-021-33632979 15002134094
- Fax
- 021-33632979
- marketing@targetmol.com
- Country
- China
- ProdList
- 7783
- Advantage
- 58
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3466
- Advantage
- 58
- Tel
- 400-164-7117 13681763483
- Fax
- +86-21-61629029
- product02@bidepharm.com
- Country
- China
- ProdList
- 41462
- Advantage
- 60
- Tel
- 027-87465837 19945049750
- Fax
- 027-8777-2287
- sales@finetechnology-ind.com
- Country
- China
- ProdList
- 9648
- Advantage
- 58
- Tel
- 021-60455363 18019463053
- Fax
- 50966098
- sales@coolpharm.com
- Country
- China
- ProdList
- 12346
- Advantage
- 58
- Tel
- +86-21-5821 5861
- Fax
- +86-21-5106 2861
- sales@letopharm.com
- Country
- China
- ProdList
- 2384
- Advantage
- 58
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4512
- Advantage
- 55
- Tel
- 021-61350663 13052117465
- Fax
- 021-61350662
- sales@zehanbiopharma.com
- Country
- China
- ProdList
- 1009
- Advantage
- 55
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 9248
- Advantage
- 55
- Tel
- 021-021-58111628 15800915896
- Fax
- QQ 3285589261
- sales@twochem.com
- Country
- China
- ProdList
- 304
- Advantage
- 55
- Tel
- 18620099427
- Fax
- +86-20-62619665
- amy@howeipharm.com
- Country
- China
- ProdList
- 17687
- Advantage
- 55
- Tel
- 021-51619050 13301662590
- Fax
- +86-21-51619052
- mandy@atkchemical.com
- Country
- China
- ProdList
- 8026
- Advantage
- 55
- Tel
- 020-61288194 61288195
- Fax
- 020-61288700
- 505721671@qq.com
- Country
- China
- ProdList
- 3866
- Advantage
- 58
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 27313
- Advantage
- 60
- Tel
- 400-1166-196 18502815961
- Fax
- QQ：800101999
- cdhxsj@163.com
- Country
- China
- ProdList
- 14603
- Advantage
- 60
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8011
- Advantage
- 62
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 7267
- Advantage
- 58
- Tel
- 021-2022843681 15618226720
- Fax
- +86-21-51601218
- lucy@atkchemical.com
- Country
- China
- ProdList
- 9204
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29785
- Advantage
- 68
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- 010-60605840 18892239720
- Fax
- 010-60605840
- psaitong@jm-bio.com
- Country
- China
- ProdList
- 12306
- Advantage
- 58
- Tel
- 0550-5196001 15000891977
- Fax
- 0550-5196001
- wj520wjxby@126.com
- Country
- China
- ProdList
- 1847
- Advantage
- 55
- Tel
- 021-58180488
- Fax
- 021-58180499
- sales@Medchemleader.com
- Country
- China
- ProdList
- 1005
- Advantage
- 58
- Tel
- 0512-56316828
- Fax
- 0512-56316826
- info@amateksci.com
- Country
- China
- ProdList
- 28810
- Advantage
- 58
- Tel
- 025-66113011 18112977050
- Fax
- 02557626880
- sales01@aikonchem.com
- Country
- China
- ProdList
- 16027
- Advantage
- 58
- Tel
- 021-54338626 18017892860
- Fax
- 021-54338626
- sales@tubepharm.com
- Country
- China
- ProdList
- 2416
- Advantage
- 58
- Tel
- 0371-0371-55051623 18137891487
- Fax
- QQ：2853979817
- 2853979817@qq.com
- Country
- China
- ProdList
- 9881
- Advantage
- 58
- Tel
- 400-9205774
- sales@glpbio.cn
- Country
- China
- ProdList
- 6777
- Advantage
- 58
- Tel
- +86-400-002-6226 +86-13028896684;
- sales@rrkchem.com
- Country
- China
- ProdList
- 57412
- Advantage
- 58
- Tel
- 15911056312
- liming@bio-fount.com
- Country
- China
- ProdList
- 9729
- Advantage
- 58
- Tel
- +86-0576-88813233 +86-13396860566
- sales@pharm-intermediates.com
- Country
- China
- ProdList
- 1990
- Advantage
- 58
- Tel
- +86-27-87465837 +8618971612321
- Fax
- 86 27 87772287
- info@finetechnology-ind.com
- Country
- China
- ProdList
- 9639
- Advantage
- 58
- Tel
- +8618530059196
- sale04@alfachem.cn
- Country
- China
- ProdList
- 13503
- Advantage
- 58
- Tel
- +1-2135480471 +1-2135480471
- sales@sarms4muscle.com
- Country
- China
- ProdList
- 10473
- Advantage
- 58
- Tel
- +8615056975894
- Fax
- 86-0551-62678551
- shawn@hirisunpharm.com
- Country
- CHINA
- ProdList
- 9911
- Advantage
- 58
- Tel
- 021-58447131 13564518121
- sales@dcchemicals.com
- Country
- China
- ProdList
- 9409
- Advantage
- 58
- Tel
- 0519-85788828 13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 3600
- Advantage
- 58
- Tel
- 13969155946
- 1461866103@qq.com
- Country
- China
- ProdList
- 16111
- Advantage
- 58
- Tel
- +86-023-6139-8061 +86-86-13650506873
- sales@chemdad.com
- Country
- China
- ProdList
- 39894
- Advantage
- 58
- Tel
- +8618523575427
- sales@conier.com
- Country
- China
- ProdList
- 49374
- Advantage
- 58
View Lastest Price from RESATORVID manufacturers
- Product
- RESATORVID 243984-11-4
- Price
- US $3.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2019-08-06