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Timegadine

Timegadine

产品编号 T13160   CAS 71079-19-1
别名: 替美加定, SR1368

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.

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Timegadine, CAS 71079-19-1
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产品目录号及名称: Timegadine (T13160)
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存储 & 溶解度
参考文献
产品描述 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.
靶点活性 COX:20 μM (in rat brain), COX:5 nM (in rabbit platelets), lipo-oxygenase:100 μM (in horse washed rabbit platelets)
体外活性 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,
体内活性 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,
别名 替美加定, SR1368
分子量 365.5
分子式 C20H23N5S
CAS No. 71079-19-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

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

参考文献

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.
Chamigrenal Murrangatin Voleneol Indomethacin sodium hydrate (S)-(+)-Ibuprofen D3 Ailanthoidol Gliotoxin Samidin

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

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

 

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