GW 6471 |
| Katalog-Nr.GC14187 |
GW 6471 ist ein potenter PPARα-Antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 880635-03-0
Sample solution is provided at 25 µL, 10mM.
GW 6471 is a potent dual PARα/γ antagonist with anti-proliferative activity in vivo and in vitro. The IC50 values of GW 6471 binding affinity to PPARα and PPARγ are 95.3 ± 42.0 nM and 39.4 ± 18.2 nM, respectively[1]. GW 6471 can be used in cancer research[1-3].
GW 6471 inhibits the growth (0.5 μM to 8 μM), migration and invasion (0.5 μM to 10 μM) of human mesothelioma cells and, at higher concentrations, reduces the viability of human mesothelioma cell line VGE62 and murine mesothelioma cell lines AB1 and AE17[1]. GW 6471 reduces HNPGL cell viability and growth by inducing cell cycle arrest and caspase-dependent apoptosis with IC50 values of 10 μM and 16 μM in PTJ64i and PTJ86i cells, respectively. The effect of GW 6471 on HNPGL cells is associated with inhibition of the PI3K/GSK3β/β-catenin signaling pathway[2].
GW 6471 (20 mg/kg) inhibited tumor growth in Caki-1 cell xenograft mouse models and the expression of c-Myc in mouse tumor tissues. No toxicity was observed at a dose of 20 mg/kg, and renal and liver functions were not adversely affected[3]. Medial prefrontal cortex injection of GW6471 (10 μg) in rats delayed the onset of the early second phase of formalin-induced nociceptive behavior[4].
References:
[1] Morales M L O, Rinaldi C A, de Jong E, et al. PPARα and PPARγ activation is associated with pleural mesothelioma invasion but therapeutic inhibition is ineffective[J]. Iscience, 2022, 25(1).
[2] Florio R, De Lellis L, di Giacomo V, et al. Effects of PPARα inhibition in head and neck paraganglioma cells[J]. PLoS One, 2017, 12(6): e0178995.
[3] Abu Aboud O, Donohoe D, Bultman S, Fitch M, Riiff T, Hellerstein M, Weiss RH. PPARα inhibition modulates multiple reprogrammed metabolic pathways in kidney cancer and attenuates tumor growth. Am J Physiol Cell Physiol. 2015 Jun 1;308(11):C890-8.
[4] Okine B N, Rea K, Olango W M, et al. A role for PPAR α in the medial prefrontal cortex in formalin‐evoked nociceptive responding in rats[J]. British journal of pharmacology, 2014, 171(6): 1462-1471.
| Cell experiment [1]: | |
Cell lines | HNPGL cells (PTJ64i and PTJ86i) |
Preparation Method | A stock solution of GW 6471 (70 mM) was prepared in DMSO, with a final DMSO concentration of 0.16% in the experiments.After incubation with GW 6471 (3 to 24 μM) for 72 hours, the cell viability was measured by MTT assay. |
Reaction Conditions | 3 to 24 μM,72 hours |
Applications | GW 6471 significantly reduced cell viability in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Caki-1 cell xenograft mouse model |
Preparation Method | After the tumor diameter reached about 5 mm, GW 6471 (20 mg/kg) was injected intraperitoneally every other day for 4 weeks. |
Dosage form | 20 mg/kg, once every two days, 4 weeks, i.p. |
Applications | GW 6471 was able to inhibit tumor growth in vivo, and GW 6471 did not adversely affect the renal and liver functions of mice. |
References: | |
| Cas No. | 880635-03-0 | SDF | |
| Chemical Name | (S,Z)-N-(3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-((4-oxo-4-(4-(trifluoromethyl)phenyl)but-2-en-2-yl)amino)propyl)propionamide | ||
| Canonical SMILES | CC1=C(N=C(C2=CC=CC=C2)O1)CCOC3=CC=C(C[C@H](N/C(C)=C\C(C4=CC=C(C(F)(F)F)C=C4)=O)CNC(CC)=O)C=C3 | ||
| Formula | C35H36F3N3O4 | M.Wt | 619.67 |
| Löslichkeit | DMF: 20 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 11 mg/ml,Ethanol: 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6138 mL | 8.0688 mL | 16.1376 mL |
| 5 mM | 0.3228 mL | 1.6138 mL | 3.2275 mL |
| 10 mM | 0.1614 mL | 0.8069 mL | 1.6138 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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