| 中文名称 |
KB-5492 free base
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| 英文名称 |
KB-5492 free base
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| 英文别名 |
1-Piperazineacetic acid, 4-[(3,4,5-trimethoxyphenyl)methyl]-, 4-methoxyphenyl ester;KB-5492 free base
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| Cas No. |
113594-64-2
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| 分子式 |
C23H30N2O6
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| 分子量 |
430.49
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
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| 详情描述 |
KB-5492 free base 是一种有效的和选择性的 sigma 受体抑制剂,抑制 [3H]1,3-di(2-tolyl)guanidine (DTG) 与 sigma 受体结合,IC50 值为 3.15 μM。KB-5492 free base 是一种抗溃疡剂。
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| 产品详情 |
KB-5492 free base 是一种有效的和选择性的 sigma 受体抑制剂,抑制 [3H]1,3-di(2-tolyl)guanidine (DTG) 与 sigma 受体结合,IC50 值为 3.15 μM。KB-5492 free base 是一种抗溃疡剂。
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| 生物活性 |
KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC 50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IC50: 3.15 μM (sigma receptor)
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| 体外研究(In Vitro) |
KB-5492 (0.001-100 μM) free base inhibits specific [H]DTG binding in a concentration-dependent manner.KB-5492 (0.1-1 mM) free base significantly and concentration-dependently prevents the ethanol- and acidified aspirin-induced increases in Cr release from gastric epithelial cells. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
KB-5492 (200?mg/kg; p.o.) free base prevents macroscopic lesions in the gastric mucosa. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Male Sprague-Dawley rats weighing 210-240 g are
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| 参考文献 |
[1]. Harada Y, et, al. Receptor binding profiles of KB-5492, a novel anti-ulcer agent, at sigma receptors in guinea-pig brain. Eur J Pharmacol. 1994 May 2; 256(3): 321-8.[2]. Morimoto Y, et, al. Effects of KB-5492, a new anti-ulcer agent, on ethanol- and acidified aspirin-induced gastric mucosal damage in vivo and in vitro. Jpn J Pharmacol. 1994 Jan; 64(1): 41-7.
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| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (232.29 mM; Need ultrasonic)配制储备液
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[1]. Harada Y, et, al. Receptor binding profiles of KB-5492, a novel anti-ulcer agent, at sigma receptors in guinea-pig brain. Eur J Pharmacol. 1994 May 2; 256(3): 321-8.[2]. Morimoto Y, et, al. Effects of KB-5492, a new anti-ulcer agent, on ethanol- and acidified aspirin-induced gastric mucosal damage in vivo and in vitro. Jpn J Pharmacol. 1994 Jan; 64(1): 41-7.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。