proglumetacin

Names

[ Name ]:
proglumetacin

[Synonym ]:
PROGLUMETACIN
Proglumetacina
Proglumetacine
3-[4-[2-[2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetyl]oxyethyl]piperazin-1-yl]propyl 4-benzamido-5-(dipropylamino)-5-oxopentanoate
Proglumetacinum

Biological Activity

[Description]:

Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV Mpro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research[1][2][3].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

[In Vitro]

Proglumetacin strongly inhibits 5-HETE formation, with an IC50 of 1.5 μM[2]. Proglumetacin inhibits leukocyte migration by inhibiting the production of the chemotactic cyclo-oxygenase product thromboxane B2[2].

[In Vivo]

Proglumetacin (Sprague-Dawley rats, 0-30 mg/kg, Orally, once) dose-dependently inhibits accumulation of pouch exudate[1]. Animal Model: Sprague-Dawley rats (6 weeks) Dosage: 0, 0.3, 3, 9, 30 mg/kg Administration: Orally, once Result: Caused dose-dependent reduction of leukocyte migration into the pouch exudate, caused 49.2% inhibition at 30 mg/kg; and markedly decreased the prostaglandin E2 content of the pouch exudate, but tended to increase the leukotriene B 4 content.

[References]

[1]. [1] NaohikoOno, et al. Effects of proglumetacin maleate and its major metabolites on allergic air pouch inflammation in rats. Eur J Pharmacol. 1987;142(2):245-251.

[2]. [2] Ono N, et al. Pharmacological studies on proglumetacin maleate, a new non-steroidal anti-inflammatory drug (4). Mode of action on anti-inflammatory activity. Japanese Journal of Pharmacology, 1986, 42(3):431-9.

[3]. [3] Alves VM, et al. QSAR Modeling of SARS-CoV Mpro Inhibitors Identifies Sufugolix, Cenicriviroc, Proglumetacin, and other Drugs as Candidates for Repurposing against SARS-CoV-2. Mol Inform. 2021 Jan;40(1):e2000113.

[4]. [4] Bozsoky S, Zahumenszky Z. A 3-month, double-blind study of proglumetacin and naproxen in the treatment of rheumatoid arthritis. Curr Med Res Opin. 1982;8(2):89-96.

Chemical & Physical Properties

[ Density]:
1.22 g/cm3

[ Boiling Point ]:
900.4ºC at 760 mmHg

[ Molecular Formula ]:
C₄₆H₅₈ClN₅O₈

[ Molecular Weight ]:
844.43

[ Flash Point ]:
498.3ºC

[ Exact Mass ]:
843.39700

[ PSA ]:
139.72000

[ LogP ]:
6.43090

[ Index of Refraction ]:
1.592

Related Compounds

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