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Technical Data
| Formula | C21H18F3NO3S2 |
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| Molecular Weight | 453.50 | CAS No. | 317318-70-0 | |
| Solubility (25°C)* | In vitro | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4. | ||
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| Targets |
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| In vitro | GW501516 is demonstrated to be 1000-fold more selective in comparison to existing subtypes. GW501516 increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts, and intestinal cells. [2] GW501516 can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. [4] Additionally, GW501516 is shown to block insulin resistance and fatty acid-induced nuclear factor-κB activation. [5] GW 501516 reduces the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity. [6] | ||
| In vivo | GW501516 dramatically increases serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. [2] GW501516 induces fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. GW501516 treatment to mice fed a high-fat diet ameliorates diet-induced obesity as well as insulin resistance. GW501516 treatment also dramatically improves diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice. [7] | ||
| Features | A selective PPARδ agonist compared with a synthetic LXRα agonist GW3965. |
Protocol (from reference)
| Animal Study:[2] |
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References
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.