Acemetacin

SKU: orb1308548

Description

Acemetacin is a carboxymethyl ester prodrug of indomethacin, a potent NSAID derived from indol-3-acetic acid. It is primarily metabolized to its active form, offering improved gastric tolerability in clinical settings. This compound is utilized in pharmacological research to study inflammation and analgesia in both in vitro and in vivo experimental models.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 53164-05-9
• MW: 415.82
• Purity: 99.98% (May vary between batches)
• Formula: C₂₁H₁₈ClNO₆
• SMILES: C(=O)(N1C=2C(C(CC(OCC(O)=O)=O)=C1C)=CC(OC)=CC2)C3=CC=C(Cl)C=C3
• Target: COX
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.81 mM);DMSO:77 mg/mL (185.18 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:54 mg/mL (129.86 mM)

Bioactivity

• Target IC50:
  COX-1:85 μM (IC50, in human intact cell)
• In Vivo:
  Acemetacin exerts its anti-inflammatory effect by inhibiting the synthesis of prostaglandins (PG). In inflamed synovial tissue, Acemetacin (10 μM) prevents the release of Prostaglandin E2 (PGE2). It inhibits the release of prostaglandin E2 in joint synovial tissues in vitro. During the incubation of gastric mucosa, the concentration-dependent inhibition of PGE accumulation by Acemetacin is not as effective as Indomethacin, and its reduction effect on gastric 6-keto-PGF1α and thromboxane B2 is also lower than that of Indomethacin.
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• In Vitro:
  In rats pre-treated with COX-2 and NOS inhibitors, despite significant inhibition of COX activity, Acemetacin significantly reduces gastrointestinal damage compared to Indomethacin.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cyclooxygenase, COX, Acemetacin, Inhibitor, K708, K-708, K 708, inhibit, TVX 1322, TVX1322, TVX-1322

Compound Identifiers

PubChem CID

1981