product name Acemetacin
Description: Acemetacin (also known as K-708) is a potent non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. 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.
References: Int J Tissue React. 1993;15(2):49-53; Methods Find Exp Clin Pharmacol. 2010 Mar;32(2):101-5.
415.82
Formula
C21H18ClNO6
CAS No.
53164-05-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 83 mg/mL (199.6 mM)
Water: <1 mg/mL
Ethanol: 58 mg/mL (139.5 mM)
Solubility (In vivo)
Synonyms
K-708
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19407734
| In Vitro |
In vitro activity: 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. Acemetacin probably exerts actions independent of conversion to Indomethacin, given the different effects of these two drugs on LTB(4) production. 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Int J Tissue React. 1993;15(2):49-53; Methods Find Exp Clin Pharmacol. 2010 Mar;32(2):101-5. |
