3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid
GW 4064
CAS: 278779-30-9
Molecular Formula: C28H22Cl3NO4
3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid - Names and Identifiers
| Name | GW 4064 |
| Synonyms | GW4064 CS-278 GW 4064 3-(2,6-Dichlorophenyl)-4-(3'-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole 3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl]Methoxy]phenyl]vinyl]benzoic acid 3-[2-[2-Chloro-4-[[3-(2,6-Dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-benzoic Acid 3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid GW 4064,3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoicacid Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-GW 4064 |
| CAS | 278779-30-9 |
| InChI | InChI=1/C28H22Cl3NO4/c1-16(2)27-21(26(32-36-27)25-22(29)7-4-8-23(25)30)15-35-20-12-11-18(24(31)14-20)10-9-17-5-3-6-19(13-17)28(33)34/h3-14,16H,15H2,1-2H3,(H,33,34)/b10-9+ |
3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid - Physico-chemical Properties
| Molecular Formula | C28H22Cl3NO4 |
| Molar Mass | 542.84 |
| Density | 1.367±0.06 g/cm3(Predicted) |
| Melting Point | >175°C (dec.) |
| Boling Point | 702.1±60.0 °C(Predicted) |
| Flash Point | 378.389°C |
| Solubility | DMSO: soluble10mg/mL, clear |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | powder |
| Color | white |
| pKa | 4.13±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.654 |
| In vitro study | GW 4064 is a complete agonist with EC50 of 80 and 90 in CV-1 cells transfected with murine and human FXR expression vectors and a defined reporter gene, respectively. GW 4064 was not active at concentrations up to 1 μm on other nuclear receptors, including the retinoic acid receptor. Therefore, GW 4064 is a potent and selective non-steroidal FXR agonist. |
| In vivo study | The pharmacokinetics of GW 4064 in rats showed that the oral bioavailability was 10%,t 1/2=3.5 hours. Fisher rats were dosed for dosing. After 7 days, serum triglycerides in GW 4064 treated rats decreased and had a dose-dependent profile, ED50 = 20 mg/kg. |
3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.842 ml | 9.211 ml | 18.422 ml |
| 5 mM | 0.368 ml | 1.842 ml | 3.684 ml |
| 10 mM | 0.184 ml | 0.921 ml | 1.842 ml |
| 5 mM | 0.037 ml | 0.184 ml | 0.368 ml |
Last Update：2024-01-02 23:10:35
3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid - Reference Information
| biological activity | GW4064 is a farnesoid X receptor (FXR) agonist, EC50 in CV1 cell line is 65 nM. When the concentration reaches 1 μM, there is no activity against other nuclear receptors. GW4064 can stimulate autophagy in MCF-7 cells. |
| target | TargetValue FXR (CV1) 65 nM(EC50) |
| Target | Value |
| FXR (CV1) | 65 nM(EC50) |
| in vitro study | GW 4064 is a complete agonist. EC50 is 80 and 90 respectively in CV-1 cells transfected with murine and human FXR expression vectors and identified reporter genes. GW 4064 is also inactive to other nuclear receptors, including retinoic acid receptors, up to a concentration of 1 μM. Therefore, GW 4064 is a strongly effective and selective non-steroidal FXR agonist. |
| in vivo study | pharmacokinetic experiments in rats showed that the oral bioavailability of GW 4064 was 10%,t 1/2=3.5 hours. Fisher rats were fed according to the dosage. After 7 days, the serum triglyceride of GW 4064 treated rats decreased and had dose-dependent characteristics, ED50 = 20 mg/kg. |
| use | an effective FXR agonist, EC50:65nM. GW-4064 is a selective agonist of FXR(EC50=15 nM). It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. GW-4064 upregulates adipokine expression in preadipocytes and HepG2 cells. GW4064 could reduce induction of proinflammatory cytokines by LPS in vitro. |
Last Update：2024-04-09 21:04:16
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Product Name: GW 4064 Visit Supplier Webpage Request for quotationCAS: 278779-30-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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