Timegadine
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (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.
For research use only. We do not sell to patients.
- CAS No.: 71079-19-1
- Formula: C20H23N5S
- Molecular Weight:365.50
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Storage:
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
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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COX 5 nM (IC50, in rabbit platelets) |
COX 20 μM (IC50, in rat brain) |
lipo-oxygenase 100 μM (IC50, in horse and washed rabbit platelets) |
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of 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[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.
Chemical Information
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CAS No. 71079-19-1
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Molecular Weight 365.50
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Formula C20H23N5S
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SMILES
CC1=NC2=CC=CC=C2C(/N=C(NC3CCCCC3)/NC4=NC=CS4)=C1
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Synonyms
SR1368
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
Female inbred Lewis rats (body weight ~150 g) are used in adjuvant arthritis and experimental allergic encephalomyelitis experiments. Paw volume is determined by mercury displacement plethismometer. Timegadine is administered orally in a volume of 1 mL/kg body weight, suspended in 0.5% carboxymethylcellulose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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