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Technical Data
| Formula | C21H20N2O5 |
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| Molecular Weight | 380.39 | CAS No. | 172732-68-2 | |
| Solubility (25°C)* | In vitro | DMSO | 76 mg/mL (199.79 mM) | |
| Ethanol | 1 mg/mL (2.62 mM) | |||
| Water | Insoluble | |||
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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 | Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3. | ||
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| In vitro | LY315920 exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50 of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively. [2] In BAL cells challenged with human sPLA2, LY315920 at doses ranging from 0.1 μM–3 μM reduces the formation of thromboxane mediated by human sPLA2 in a concentration-dependent manner with an IC50 of approximately 0.8 μM. [2] In human conjunctival epithelial cell line (HCjE), LY315920 (10 μM) significantly inhibits all-trans-retinoic acid (RA) -induced membrane-associated mucin MUC16 expression by 100% at 24 hours and 99% at 48 hours. [3] | ||
| In vivo | Ex vivo, LY315920 at doses ranging from 3 mg/kg to 30 mg/kg via i.v. inhibits human sPLA2-induced release of thromboxane from guinea pig BAL cells with ED50 of 16.1 mg/kg. [2] In Transgenic Mice Expressing Human sPLA2, both oral and i.v. administration of LY315920 (0.3 mg/kg–3 mg/kg) abolishes serum sPLA2 activity in a dose and time dependent manner. [2] | ||
| Features | A potent and selective secretory phospholipase A2 inhibitor. |
Protocol (from reference)
| Animal Study:[2] |
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References
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Customer Product Validation
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, , J Am Heart Assoc, 2015, 4:e002553.
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, , PLoS One, 2015, 10(4):e0119088.
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Data from [Data independently produced by , , Mol Cancer, 2013, 12(1):111.]
Selleck's Varespladib (LY315920) has been cited by 11 publications
| Exploring Lysophosphatidylcholine as a Biomarker in Ischemic Stroke: The Plasma-Brain Disjunction [ Int J Mol Sci, 2024, 25(19)10649] | PubMed: 39408978 |
| The Candida albicans toxin candidalysin mediates distinct epithelial inflammatory responses through p38 and EGFR-ERK pathways [ Front Immunol, 2022, 13:824746] | PubMed: 35392090 |
| Substrate-Specific Inhibition Constants for Phospholipase A2 Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics [ J Med Chem, 2019, 62(4):1999-2007] | PubMed: 30615445 |
| Substrate-Specific Inhibition Constants for Phospholipase A2 Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics [ J Med Chem, 2019, 62(4):1999-2007] | PubMed: 30615445 |
| Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376] | PubMed: 30046109 |
| Novel Role for Matrix Metalloproteinase 9 in Modulation of Cholesterol Metabolism [ J Am Heart Assoc, 2016, 5(10)e004228] | PubMed: 27694328 |
| Identification of a Novel Heart–Liver Axis: Matrix Metalloproteinase-2 Negatively Regulates Cardiac Secreted Phospholipase A2 to Modulate Lipid Metabolism and Inflammation in the Liver [Hernandez-Anzaldo S, et al. J Am Heart Assoc, 2015, 4:e002553] | PubMed: 26567374 |
| Matrix metalloproteinase-2 negatively regulates cardiac secreted phospholipase A2 to modulate inflammation and Fever. [Berry E, et al. J Am Heart Assoc, 2015, 4(4)] | PubMed: 25820137 |
| Cytosolic Phospholipase A2 Modulates TLR2 Signaling in Synoviocytes [Sommerfelt RM, et al. PLoS One, 2015, 10(4):e0119088] | PubMed: 25893499 |
| Novel role of group VIB Ca2+-independent phospholipase A2F in leukocyte-endothelial cell interactions: An intravital microscopic study in rat mesentery [Kojima M, et al. J Trauma Acute Care Surg, 2015, 79(5):782-9] | PubMed: 26496102 |
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.