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].
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- CAS No.: 57132-53-3
- 화학식: C46H58ClN5O8
- 분자량:844.43
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (6 weeks)
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Dosage:0, 0.3, 3, 9, 30 mg/kg
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Administration:Orally, once
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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.
Chemical Information
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CAS No. 57132-53-3
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분자량 844.43
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화학식 C46H58ClN5O8
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SMILES
O=C(CC1=C(C)N(C(C2=CC=C(C=C2)Cl)=O)C3=C1C=C(C=C3)OC)OCCN4CCN(CCCOC(CCC(C(N(CCC)CCC)=O)NC(C5=CC=CC=C5)=O)=O)CC4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Proglumetacin Related Classifications
HY-106560 Related Classifications
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