Introduction：Basic information about CAS 57132-53-3|proglumetacin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| 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 | / |
|---|
| MSDS | / | Flash Point | 498.3ºC |
|---|
Names
| Name | proglumetacin |
|---|
| Synonym | More Synonyms |
|---|
proglumetacin BiologicalActivity
| 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 |
|---|
| InChIKey | PTXGHCGBYMQQIG-UHFFFAOYSA-N |
|---|
| SMILES | CCCN(CCC)C(=O)C(CCC(=O)OCCCN1CCN(CCOC(=O)Cc2c(C)n(C(=O)c3ccc(Cl)cc3)c3ccc(OC)cc23)CC1)NC(=O)c1ccccc1 |
|---|
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 |
