3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE
2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride
CAS: 405911-17-3
Molecular Formula: C33H31ClF3NO3.HCl
3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE - Names and Identifiers
3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C33H31ClF3NO3.HCl |
| Solubility | DMSO : 70 mg/mL (ultrasonic) Mother Liquor Preservation: Sub-packing and freezing to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, as far as possible) Cell experiment: Dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to co |
| Appearance | powder |
| Color | white |
| Storage Condition | -20°C |
| MDL | MFCD08276920 |
| Use | GW-3965 is a liver X receptor agonist. GW3965 represses the production of pro-inflammatory cytokines by murine mast cells. GW3965 improves recovery from mild repetitive traumatic brain injury in mice partly through apolipoprotein E. GW3965 reduces tissue factor production and inflammatory responses in human islets in vitro. GW3965 dose-dependently regulates lps-mediated liver injury and modulates posttranscriptional TNF-alpha production and p38 mitogen-activated protein kinase activation in liver macrophages. |
| Target | hLXRα;hLXRβ;LXRα/SRC1 LiSA |
| In vitro study | GW3965 aggregates steroid receptor coactivator 1 to lxrα with an EC50 of 125 nM in the cell-free Ligand Detection Assay. GW3965 exhibited potent antagonistic activity against hLXR α and hLXR β with EC50 of 190 nM and 30 nM, respectively, in the cell assay. In addition, GW3965 also showed excellent selectivity for other nuclear receptors. In human islets, GW3965 (1 μm) reduced the expression of selected pro-inflammatory cytokines, including IL-8, monocyte chemoattractant protein -1 and tissue factor. |
| In vivo study | In mice, GW3965 at a dose of 10 mg/kg up-regulates ABCA1 expression by 8-fold and increases circulating levels by 30% with a C max of 12.7 μg/mL ,t 1/2 is 2 hours. In LDLR −/− and apoE −/− mice, GW3965 (10mg/kg) induced ABCA1 and ABCG1 expression and exhibited potent anti-atherosclerotic activity. GW3965 reduced Ang II-mediated increase in blood pressure and reduced vascular Ang II receptor gene expression in male sprague-dawley rats. In a mouse model of malignant glioma, GW3965 leads to degradation of LDLR and increases the expression of ABCA1 cholesterol efflux transporter, thereby effectively promoting tumor cell death. |
3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R41 - Risk of serious damage to eyes |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S39 - Wear eye / face protection. |
| WGK Germany | 3 |
3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE - Reference
| Reference Show more | 1: Wang R, Li R, Wen Q, Peng K, Tan X, Chen Z. [Expression of LXR-β in human gastric cancer tissue and the effect of GW3965 on the proliferation of gastric cancer cell line SGC-7901]. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2016 Feb 28;41(2):127-33. doi: 10.11817/j.issn.1672-7347.2016.02.003. Chinese. PubMed PMID: 26932209. 2: Nunomura S, Okayama Y, Matsumoto K, Hashimoto N, Endo-Umeda K, Terui T, Makishima M, Ra C. Activation of LXRs using the synthetic agonist GW3965 represses the production of pro-inflammatory cytokines by murine mast cells. Allergol Int. 2015 Sep;64 Suppl:S11-7. doi: 10.1016/j.alit.2015.03.001. Epub 2015 Mar 31. PubMed PMID: 26344074. 3: Archer A, Stolarczyk E, Doria ML, Helguero L, Domingues R, Howard JK, Mode A, Korach-André M, Gustafsson JÅ. LXR activation by GW3965 alters fat tissue distribution and adipose tissue inflammation in ob/ob female mice. J Lipid Res. 2013 May;54(5):1300-11. doi: 10.1194/jlr.M033977. Epub 2013 Feb 27. PubMed PMID: 23446231; PubMed Central PMCID: PMC3622325. 4: Namjoshi DR, Martin G, Donkin J, Wilkinson A, Stukas S, Fan J, Carr M, Tabarestani S, Wuerth K, Hancock RE, Wellington CL. The liver X receptor agonist GW3965 improves recovery from mild repetitive traumatic brain injury in mice partly through apolipoprotein E. PLoS One. 2013;8(1):e53529. doi: 10.1371/journal.pone.0053529. Epub 2013 Jan 17. PubMed PMID: 23349715; PubMed Central PMCID: PMC3547922. 5: Cui X, Chopp M, Zacharek A, Cui Y, Roberts C, Chen J. The neurorestorative benefit of |
3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.617 ml | 8.084 ml | 16.168 ml |
| 5 mM | 0.323 ml | 1.617 ml | 3.234 ml |
| 10 mM | 0.162 ml | 0.808 ml | 1.617 ml |
| 5 mM | 0.032 ml | 0.162 ml | 0.323 ml |
Last Update：2024-01-02 23:10:35
3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE - Cell Experiment
Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37ºC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays.
Last Update：2023-08-16 21:32:38
3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE - Introduction
2-(3-(3-((2-chroo-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride is a compound, its chemical name is 1-(4-(2-(3-(4-chroophenyl) propoxy)-5-methylpyrimidin-4-yl)phenyl)-3-(4-(phenyl) phenyl)urea hydrochloride. It is a fatty acid receptor activator (fatty acid receptor agonist), which is widely used in biomedical research.
2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride is mainly used to activate the nuclear receptor transcription factor LXR(liver X receptor), thereby regulating cholesterol and lipid metabolism. LXR is a transcription factor that regulates cholesterol synthesis and transport by activating LXR,2-(3-((2-chroo-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride can affect lipid metabolism pathways and has a variety of biological activities such as anti-inflammatory, antioxidant and anti-tumor.
Preparation of 2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenyl ethyl)amino)propoxy)phenyl) the method of acetic acid hydrochloride is generally a synthetic organic synthetic route. First, the precursor compound of GW3965 is synthesized by chemical method, and then 2-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2) is formed by adding HCl acid, 2-diphenyl ethyl)amino)propoxy)phenyl)acetic acid hydrochloride.
2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride has limited safety information. When using it, you should follow the laboratory safety procedures and strictly control the dosage. In addition, 2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenyl ethyl)amino)propoxy)phenyl)acetic acid hydrochloride should be stored in a dry, cool place, avoid light and damp. When used, avoid inhalation, ingestion or contact with skin and eyes. In case of accidental contact, rinse immediately with plenty of water and seek medical help.
2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride is mainly used to activate the nuclear receptor transcription factor LXR(liver X receptor), thereby regulating cholesterol and lipid metabolism. LXR is a transcription factor that regulates cholesterol synthesis and transport by activating LXR,2-(3-((2-chroo-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride can affect lipid metabolism pathways and has a variety of biological activities such as anti-inflammatory, antioxidant and anti-tumor.
Preparation of 2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenyl ethyl)amino)propoxy)phenyl) the method of acetic acid hydrochloride is generally a synthetic organic synthetic route. First, the precursor compound of GW3965 is synthesized by chemical method, and then 2-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2) is formed by adding HCl acid, 2-diphenyl ethyl)amino)propoxy)phenyl)acetic acid hydrochloride.
2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride has limited safety information. When using it, you should follow the laboratory safety procedures and strictly control the dosage. In addition, 2-(3-(3-((2-choro-3-(trifluoromethyl)benzyl)(2,2-diphenyl ethyl)amino)propoxy)phenyl)acetic acid hydrochloride should be stored in a dry, cool place, avoid light and damp. When used, avoid inhalation, ingestion or contact with skin and eyes. In case of accidental contact, rinse immediately with plenty of water and seek medical help.
Last Update：2024-04-09 21:01:54
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3-[3-[[[2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]METHYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY]BENZENEACETIC ACID HYDROCHLORIDE
2,6-dinitro-p-toluidine
3-Isoproproxy-4-methylphenylboronic acid pinacol ester
依托必利碱
甲萘酚硫酸钠
AMMONIUM TITANYL OXALATE
C.I.Vat Red 15
TOSLAB 837277
4-甲氧基呋喃并[3,2-D]嘧啶-6-羧酸
地美罗酸镁盐
2,6-dinitro-p-toluidine
3-Isoproproxy-4-methylphenylboronic acid pinacol ester
依托必利碱
甲萘酚硫酸钠
AMMONIUM TITANYL OXALATE
C.I.Vat Red 15
TOSLAB 837277
4-甲氧基呋喃并[3,2-D]嘧啶-6-羧酸
地美罗酸镁盐