GW0742 (Synonyms: GW 0742) |
| Katalog-Nr.GC14983 |
A selective agonist of PPARδ
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 317318-84-6
Sample solution is provided at 25 µL, 10mM.
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GW0742 is a synthetic, potent, and selective PPAR-β/δ agonist. PPARs are ligand-dependent transcription factors that are involved in many physiological processes, such as inflammation and energy homeostasis. PPAR-β/δ is one of three PPARs in the nuclear hormone receptor superfamily that are collectively involved in the control of lipid homeostasis among other functions. GW0742 can attenuate the increase of PARP activity caused by SAO shock. GW0742 is also able to prevent radiation-induced brain injury in C57Bl/6 wild-type (WT) and PPARδ knockout (KO) mice. Dietary GW0742 can prevent the acute increase in IL-1β mRNA and ERK phosphorylation measured at 3 h after a single 10-Gy dose of WBI as well as the rise in the number of activated hippocampal microglia 1 week after WBI.
References:
[1].Rosanna Di Paola, Emanuela Esposito, Emanuela Mazzon, Irene Paterniti, Maria Galuppo, Salvatore Cuzzocrea. GW0742, a selective PPAR-β/δ agonist, contributes to the resolution of inflammation after gut ischemia/reperfusion injury. August 2010. Journal of Leukocyte Biology. vol. 88 no. 2 291-301
[2].Caroline I. Schnegg, Dana Greene-Schloesser, Mitra Kooshki, Valerie S. Payne, Fang-Chi Hsud, Mike E. Robbins. hippocampal-dependent cognitive impairment after whole-brain irradiation. Free Radical Biology and Medicine. Volume 61, August 2013, Pages 1–9.
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Cell experiment: |
The PPARβ activator GW0742 and the RXR activator 9-cis-retinoic acid are dissolved in DMSO. The final DMSO concentration des not exceed 0.5% v/v, and this concentration is used in control wells. For each culture plate, one row of wells is treated with 500 μM glutamate. These wells serve as a positive control and for normalisation of data. Cell death (toxicity) is assessed by using an assay designed to measure lactate dehydrogenase (LDH) release[2]. |
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Animal experiment: |
Male CD mice (25-35 g) are housed in a controlled environment and provided with standard rodent chow and water. Mice are randomized into four experimental groups: bleomycin-treated group: mice are subjected to lung injury induced by intratracheal instillation of bleomycin and treated daily via intraperitoneal injection with vehicle of GW0742 (10% dimethylsulfoxide (OMSO, 1 mL/kg), 1 h after BLEO instillation (n = 15). GW0742 group: identical to bleomycin-treated group but mice are treated daily with GW0742 (0.3 mg/kg, 1h after BLEO instillation) via intraperitoneal injection (n = 15). Sham-operated mice + vehicle group: animals are subjected to the identical surgical procedure but receive intratracheal instillation of saline (0.9%) instead of BLEO and are treated daily with the vehicle of GW0742 (10% dimethylsulfoxide (DMSO), 1 mL/kg, i.p.), 1 h after saline instillation (n = 15). Sham-operated mice + GW0742 group: identical to sham + vehicle group but mice are treated daily with GW0742 (0.3 mg/kg, 1 h after saline instillation) via intraperitoneal injection (n = 15)[3]. |
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References: [1]. Sznaidman ML, et al. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21. |
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| Cas No. | 317318-84-6 | SDF | |
| Überlieferungen | GW 0742 | ||
| Chemical Name | 2-[4-[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methylsulfanyl]-2-methylphenoxy]acetic acid | ||
| Canonical SMILES | CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC(=C(C=C3)C(F)(F)F)F)C)OCC(=O)O | ||
| Formula | C21H17F4NO3S2 | M.Wt | 471.49 |
| Löslichkeit | ≥ 47.1 mg/mL in DMSO, ≥ 49.7 mg/mL in EtOH with ultrasonic and warming | 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 | 2.1209 mL | 10.6047 mL | 21.2094 mL |
| 5 mM | 0.4242 mL | 2.1209 mL | 4.2419 mL |
| 10 mM | 0.2121 mL | 1.0605 mL | 2.1209 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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