| CAS NO: | 53164-05-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1g | 询价 |
| 2g | 询价 |
| 5g | 询价 |
| 10g | 询价 |
| 25g | 询价 |
| 50g | 询价 |
| 100g | 询价 |
| Molecular Weight (MW) | 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) | |
| Other info | Chemical Name: 1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, carboxymethyl ester InChi Key: FSQKKOOTNAMONP-UHFFFAOYSA-N InChi Code: InChI=1S/C21H18ClNO6/c1-12-16(10-20(26)29-11-19(24)25)17-9-15(28-2)7-8-18(17)23(12)21(27)13-3-5-14(22)6-4-13/h3-9H,10-11H2,1-2H3,(H,24,25) SMILES Code: O=C(OCC(O)=O)CC1=C(C)N(C(C2=CC=C(Cl)C=C2)=O)C3=C1C=C(OC)C=C3 |
| Synonyms | TVX1322; K-708; Acemetacin; Rantudil; K 708; TVX 1322; TVX-1322; K708 |
| 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. |
|---|---|
| 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 | Rats |
| Formulation & Dosage | N/A |
| References | Int J Tissue React. 1993;15(2):49-53; Methods Find Exp Clin Pharmacol. 2010 Mar;32(2):101-5. |
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