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Timegadine

Catalog No. T13160   CAS 71079-19-1
Synonyms: SR1368

Timegadine is a competitive inhibitor of <a href="/target/COX" style="display: inline; color: #c13a36">COX</a> and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for <a href="/target/COX" style="display: inline; color: #c13a36">COX</a> and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates and in washed rabbit platelets.

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Timegadine, CAS 71079-19-1
Pack Size Availability Price/USD Quantity
5 mg 8-10 weeks $ 970.00
50 mg 8-10 weeks $ 1,980.00
100 mg 8-10 weeks $ 2,500.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Timegadine is a competitive inhibitor of COX and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates and in washed rabbit platelets.
Targets&IC50 COX:20 μM (in rat brain), COX:5 nM (in rabbit platelets), lipo-oxygenase:100 μM (in horse washed rabbit platelets)
In vitro Timegadine is a potent, competitive COX and lipo-oxygenase inhibitor, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets[2],and is a new antiinflammatory agent,
In vivo Timegadine is a potent, competitive prostaglandin synthetase inhibitor which also inhibits cyclo-oxygenase (COX) and lipoxygenase. Daily oral doses of 10 to 30 mg/kg of Timegadine significantly inhibit both the primary and secondary lesions of adjuvant arthritis when the treatment is initiated on the day of the disease induction and continues for 28 days. Timegadine is able specifically to prevent the development of the swelling of the non-injected paw until 28 days after the adjuvant injection when administered for 5 days prior to and 5 days after the induction of the disease, in analogy with the effect of cyclophosphamide[1].Timegadine is a new antiinflammatory agent,
Synonyms SR1368
Molecular Weight 365.5
Formula C20H23N5S
CAS No. 71079-19-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. George S, et al. The influence of food intake on the bioavailability of timegadine, a novel non-steroidal anti-inflammatory drug. Br J Clin Pharmacol. 1983 Apr;15(4):495-8. 2. Ahnfelt-Rønne I, et al. A new antiinflammatory compound, timegadine (N-cyclohexyl-N"-4-[2-methylquinolyl]-N'-2-thiazolylguanidine), which inhibits both prostaglandin and 12-hydroxyeicosatetraenoic acid (12-HETE) formation. Biochem Pharmacol. 1980 Dec;29(24):3265-9.

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Keywords

Timegadine 71079-19-1 Immunology/Inflammation Neuroscience COX SR1368 Inhibitor inhibitor inhibit