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  3. Timegadine

Timegadine  (Synonyms: 替美加定; SR1368)

目录号: HY-100125
产品使用指南

Timegadine 是一种新的抗炎药,被发现是一种有效的竞争性前列腺素合成酶抑制剂,同时也能抑制环加氧酶和脂氧合酶。

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Timegadine Chemical Structure

Timegadine Chemical Structure

CAS No. : 71079-19-1

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target

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)

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of prostaglandin synthetase 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

365.50

Formula

C20H23N5S

CAS 号
中文名称

替美加定

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Timegadine 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Timegadine
目录号:
HY-100125
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