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Acemetacin COX inhibitor

Cat.No.S2602

Acemetacin (K-708,TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
Acemetacin COX inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 415.82

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Quality Control

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 415.82 Formula

C21H18ClNO6

 Storage (From the date of receipt)
CAS No. 53164-05-9 Download SDF Storage of Stock Solutions

Synonyms K-708,TVX 1322 Smiles CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)OCC(=O)O

Mechanism of Action

Targets/IC50/Ki
COX
In vitro

Acemetacin is less potent than indomethacin in causing a concentration-related inhibition of PGE accumulation in gastric mucosal incubates. This compound is also less potent than indomethacin in reducing gastric 6-keto-PGF1 alpha and TXB2. It probably exerts actions independent of conversion to Indomethacin, given the different effects of these two drugs on LTB(4) production. This prodrug of indomethacin exhibits better gastric tolerability in preclinical and clinical trials. It involves the sequential participation of nitric oxide (NO) or K+ channel pathways to confer its antinociceptive effect. This compound exhibits the anti-inflammatory effect through PG synthesis inhibition. It prevents the PGE2 release only at the high concentration of 10 μM in inflamed synovial tissue. This chemical exhibits less potent inhibitory effect on PGE2 release from the synovial membrane in the in vitro study.

In vivo

This compound induces significantly less gastric and intestinal damage than indomethacin in rats pretreated with inhibitors of COX-2 and NOS, despite markedly suppressing COX activity.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/6587139/
  • [5] https://pubmed.ncbi.nlm.nih.gov/20401346/

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