| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
GW7647 (GW-7647) is a novel, selective and potent agonist of human and murine PPARα4 with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively. It was identified by assaying it for activity on human PPAR subtypes and employing solid-phase, parallel-array synthesis. Strong lipid-lowering activity in animal models of dyslipidemia was found for GW7647, a human PPARalpha agonist with about 200-fold selectivity over PPARgamma and PPARdelta. GW7647 is going to be a very useful chemical tool for researching the biology of PPARalpha in disease models in animals and human cells.
| Targets |
PPARα (EC50 = 6 nM); Chk2 (IC50 = 697.4 nM); PPARγ (EC50 = 1.1 μM); PPARδ (EC50 = 6.2 μM)
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| ln Vitro |
GW7647 (1 μM) causes both in the presence and absence of IL-1β a significant increase in PDZK1 protein expression in Caco2BBE cells, reaching 129.7 ± 6.5% of vehicle treated control[1]. GW7647 also attenuates the PDZK1 expression decrease mediated by IL-1β.
GW7647 (50 nM) increases the amounts of NO released by stimulating the phosphorylation of PI3K and then Akt (Ser473) in the stripped antral mucosa. In antral mucous cells, GW7647 (50 nM) amplifies the first stage of Ca2+-regulated exocytotic events triggered by ACh, but GW7647 by itself does not cause any exocytotic events. In antral mucous cells, GW7647 plus ACh increases the effects of wortmannin (50 nM) and AKT-inh (100 nM) on exocytotic events[2]. GW 7647 (100 nM) decreases the AQP9 protein abundance by 43%; however, at 10 and 1,000 nM, it has no discernible effec in WIF-B9 hepatocytes. HepG2 cells exposed to GW 7647 (100 nM) exhibit a 24% decrease in AQP9 protein abundance; however, L-FABP protein abundance in HepG2 hepatocytes is not significantly increased[3]. |
| ln Vivo |
GW7647 (3 mg/kg per day) inhibits the decrease in left ventricular ejection fraction but does not stop the development of cardiac hypertrophy in vivo[4].
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| Animal Protocol |
New Zealand newborn Seven-day-old white rabbits weighing between 90 and 200 grams are anesthetized with 2% isofluorane inhaled, and they undergo an aorto-caval shunt to cause volume-overload cardiac hypertrophy. When using a color flow doppler on postoperative days 7 and 13, it is possible to see a physical shunt between the inferior vena cava and the abdominal aorta in both the axial and transverse planes, indicating the presence of a successful fistula. The enlarged inferior vena cava serves as additional confirmation of this. Following validation, animals in the shunt group are randomized to receive either GW7647 (3 mg/kg per day; EC50=6 nM for PPARα) or the vehicle (dimethyl sulfoxide, the solvent of GW7647) twice daily for 14 days via intraperitoneal injection. Animals that have surgery to create a shunt are not allowed to continue in the study if the shunt closes or does not exhibit. Transthoracic echocardiography is used to measure the left ventricular ejection fraction (%) and other cardiac parameters on postoperative days 7 and 13. All animals are put to sleep with Na+ pentobarbital at age 21 (14 days after surgery), and their hearts are removed for isolated biventricular working heart perfusions.
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| References |
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| Molecular Formula |
C29H46N2O3S
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|---|---|
| Molecular Weight |
502.75214
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| Exact Mass |
502.32
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| Elemental Analysis |
C, 69.28; H, 9.22; N, 5.57; O, 9.55; S, 6.38
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| CAS # |
265129-71-3
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| Related CAS # |
265129-71-3
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| Appearance |
White to off-white solid powder
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| SMILES |
CC(C)(C(=O)O)SC1=CC=C(C=C1)CCN(CCCCC2CCCCC2)C(=O)NC3CCCCC3
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| InChi Key |
PKNYXWMTHFMHKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H46N2O3S/c1-29(2,27(32)33)35-26-18-16-24(17-19-26)20-22-31(28(34)30-25-14-7-4-8-15-25)21-10-9-13-23-11-5-3-6-12-23/h16-19,23,25H,3-15,20-22H2,1-2H3,(H,30,34)(H,32,33)
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| Chemical Name |
2-[4-[2-[4-cyclohexylbutyl(cyclohexylcarbamoyl)amino]ethyl]phenyl]sulfanyl-2-methylpropanoic acid
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| Synonyms |
GW 7647; GW-7647; GW7647
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~198.9 mM)
Ethanol: ~25 mg/mL (~49.7 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.97 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 (4.97 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9891 mL | 9.9453 mL | 19.8906 mL | |
| 5 mM | 0.3978 mL | 1.9891 mL | 3.9781 mL | |
| 10 mM | 0.1989 mL | 0.9945 mL | 1.9891 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.
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