proglumetacin

Modify Date: 2024-01-13 18:44:38

proglumetacin Structure
proglumetacin structure
Common Name proglumetacin
CAS Number 57132-53-3 Molecular Weight 844.43
Density 1.22 g/cm3 Boiling Point 900.4ºC at 760 mmHg
Molecular Formula C46H58ClN5O8 Melting Point N/A
MSDS N/A Flash Point 498.3ºC

 Use of proglumetacin


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].

 Names

Name proglumetacin
Synonym More Synonyms

 proglumetacin 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
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

 Synonyms

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