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Technical Data
| Formula | C16H11Cl2FO2 |
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| Molecular Weight | 325.16 | CAS No. | 749269-83-8 | |
| Solubility (25°C)* | In vitro | DMSO | 65 mg/mL (199.9 mM) | |
| Ethanol | 12 mg/mL (36.9 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 | Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L. | |
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| Targets |
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| In vitro | In human neuroglioma cells over-expressing the Swedish mutated APP [human neuroglioma cell line expressing APPswe (H4swe)], CHF5074 preferentially lowers Aβ42 secretion with an IC50 of 3.6 µmol/L. CHF5074 does not display inhibitory activity on COX-1 and COX-2 enzymes when employed at concentrations up to 100 µmol/L and 300 µmol/L respectively[1]. |
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| In vivo | In rats, CHF5074 is orally well absorbed (50%) and is slowly eliminated from plasma (t1/2 ≈ 20 h). In Tg2576 transgenic mice, chronic treatment with CHF5074 markedly reduces brain Aβ burden without histological signs of peripheral Notch-mediated toxicity[1]. |
Protocol (from reference)
RETURN POLICY
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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.