| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
GW0742 (GW-0742; GW 0742; GW-0742X; GW0742X; GW610742; GW-610742) is a potent and highly selective PPARβ/δ agonist with potential anti-inflammatory activity. It acts by activating PPAR with an IC50 of 1 nM, and exhibits >1000-fold selectivity for PPARβ/δ over PPARα and PPARγ.
| ln Vitro |
GW0742 is a strong PPARβ and PPARδ agonist, having an IC50 of 1 nM for human PPARδ and EC50s of 1 nM, 1.1 μM, and 2 μM for human PPARδ, PPARα, and PPARγ, respectively[1]. In MCF-7 cells, GW0742 (100 μM) activates both murine and human PPARβ. Cerebellar granule neurons that are driven to undergo apoptosis by low KCl had their apoptosis greatly reduced by GW0742 (100 μM). GW0742 causes more cell death at 100 μM after 48 hours of treatment, but it does not appear to have any discernible intrinsic toxicity on cerebellar granule neuronal cells treated at 3-100 μM for 24 hours. Furthermore, it has been observed that GW0742 (100 μM) elevates c-Jun expression in cultures of cerebellar granule neurons after 6 hours[2]. In neonatal rat cardiomyocytes, GW0742 (1 μM) induces the expression of PPARδ protein. In newborn rat cardiomyocytes, GW0742 also increases the mRNA levels of malonyl-CoA decarboxylase (MCD), pyruvate dehydrogenase kinase 4 (PDK4), acyl-CoA oxidase 1 (ACOX1), long-chain acyl-CoA dehydrogenase (LCAD), and very long-chain acyl-CoA dehydrogenase (VLCAD), acyl-CoA oxidase 1 (ACOX1), uncoupling protein 3 (UCP3), and malonyl-CoA decarboxylase (MCD[4].
|
||
|---|---|---|---|
| ln Vivo |
In mice with lung injury generated by bleomycin instilllatio (BLEO), GW0742 (0.3 mg/kg, ip) attenuates the histological indications and decreases the intensity of masson-trichrome staining. In addition, GW0742 (0.3 mg/kg, ip) lowers myeloperoxidase (MPO) activity and the body weight loss caused by BLEO. Instilled mice with GW0742 exhibit a notable reduction in TNF-a and IL-1β levels. In BLEO-induced mice, GW0742 inhibits bleomycin-induced IkB-a degradation, lowers lung NF-kB p65 levels, and lowers iNOS and p-ERK expression[3]. Rat cardiac tissue exposed to GW0742 (5 mg/kg/day, IV) has elevated PPARδ protein levels. Additionally, GW0742 causes an increase in VLCAD, ACOX1, and LCAD in rat hearts[4].
|
||
| Animal Protocol |
|
||
| 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.
[2]. Smith SA, et al. Effect of the peroxisome proliferator-activated receptor beta activator GW0742 in rat cultured cerebellar granule neurons. J Neurosci Res. 2004 Jul 15;77(2):240-9. [3]. Galuppo M, et al. GW0742, a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice. Int J Immunopathol Pharmacol. 2010 Oct-Dec;23(4):1033-46. [4]. Kuo SC, et al. Activation of receptors δ (PPARδ) by agonist (GW0742) may enhance lipid metabolism in heart both in vivo and in vitro. Horm Metab Res. 2013 Nov;45(12):880-6 |
| Molecular Formula |
C21H17F4NO3S2
|
|
|---|---|---|
| Molecular Weight |
471.49
|
|
| CAS # |
317318-84-6
|
|
| Related CAS # |
|
|
| SMILES |
O=C(O)COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C(F)=C3)S2)C=C1C
|
|
| InChi Key |
HWVNEWGKWRGSRK-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C21H17F4NO3S2/c1-11-7-14(4-6-17(11)29-9-19(27)28)30-10-18-12(2)26-20(31-18)13-3-5-15(16(22)8-13)21(23,24)25/h3-8H,9-10H2,1-2H3,(H,27,28)
|
|
| Chemical Name |
[4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methyl phenoxy]-acetic acid
|
|
| Synonyms |
GW-0742X; GW-610742; GW0742; GW-0742; GW 0742X; GW610742; GW 0742; GW0742X; GW 610742
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|---|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
