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Technical Data
| Formula | C21H18ClNO6 |
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| Molecular Weight | 415.82 | CAS No. | 53164-05-9 | |
| Solubility (25°C)* | In vitro | DMSO | 83 mg/mL (199.6 mM) | |
| Ethanol | 83 mg/mL (199.6 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 | Acemetacin (K-708,TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. | |
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| In vitro | Acemetacin is less potent than indomethacin in causing a concentration-related inhibition of PGE accumulation in gastric mucosal incubates. Acemetacin is also less potent than indomethacin in reducing gastric 6-keto-PGF1 alpha and TXB2. [1] Acemetacin probably exerts actions independent of conversion to Indomethacin, given the different effects of these two drugs on LTB(4) production. [2] Acemetacin is a prodrug of indomethacin that exhibits better gastric tolerability in preclinical and clinical trials. Acemetacin involves the sequential participation of nitric oxide (NO) or K+ channel pathways to confer its antinociceptive effect. [3] Acemetacin exhibits the anti-inflammatory effect through PG synthesis inhibition. Acemetacin prevents the PGE2 release only at the high concentration of 10 μM in inflamed synovial tissue. Acemetacin exhibits less potent inhibitory effect on PGE2 release from the synovial membrane in the in vitro study. [4] |
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| In vivo | Acemetacin induces significantly less gastric and intestinal damage than indomethacin in rats pretreated with inhibitors of COX-2 and NOS, despite markedly suppressing COX activity. [5] |
Protocol (from reference)
References
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.