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Technical Data
| Formula | C17H17N5O |
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| Molecular Weight | 307.35 | CAS No. | 874902-19-9 | |
| Solubility (25°C)* | In vitro | DMSO | 61 mg/mL (198.47 mM) | |
| Ethanol | 61 mg/mL (198.47 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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Preparing Stock Solutions
Biological Activity
| Description | LY-2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH). LY-2183240 disrupts the cellular uptake of the lipid endocannabinoid (EC) anandamide and promote analgesia in vivo. LY-2183240 is also an inhibitor of monoacylgylcerol lipase (MGL). | ||
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| Targets |
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Biological Activity
| Description | LY-2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH). LY-2183240 disrupts the cellular uptake of the lipid endocannabinoid (EC) anandamide and promote analgesia in vivo. LY-2183240 is also an inhibitor of monoacylgylcerol lipase (MGL). | ||
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| Targets |
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| In vitro | LY2183240 inhibits anandamide uptake in live cell with IC50 of 0.27 nM. [1] LY2183240 inactivates FAAH by carbamylation of the enzyme’s serine nucleophile. LY2183240 also inhibits KIAA1363, α/β-hydrolase 6 (Abh6) and monoacylglycerol lipase (MAG lipase) expressed in COS-7 cells with IC50 of 8.3, 0.09 and 5.3 nM, respectively. [2] |
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| In vivo | LY2183240 (i.p.) results in a dose-dependent increase in anandamide concentrations in rat cerebellum with ED50 of 1.37 mg/kg. LY2183240 (i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms. [1] LY2183240 (10 mg/kg, i.p.) treatment for 90 min inactivates FAAH (100% inhibited), Abh6 (>90% inhibited), and MAG lipase (>60% inhibited) in brain tissue. [2] LY2183240 shows beneficiation on fear-potentiated startle (FPS) and alcohol-seeking behaviors (HAP) in mice selectively bred for high alcohol preference. Repeated administration of LY2183240 (30 mg/kg) reduces the expression of FPS in HAP mice when given prior to a second FPS test 48 h after fear conditioning. Both the 10 and 30 mg/kg doses of LY2183240 enhances the expression of alcohol-induced conditioned place preference and this effect persisted in the absence of the drug. [3] |
Protocol (from reference)
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References
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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.