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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Zaltoprofen
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
74711-43-6
- 规格：
1mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥200.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥290.0 |
| 规格： | 10mg | 产品价格： | ￥420.0 |
| 规格： | 25mg | 产品价格： | ￥670.0 |
| 规格： | 50mg | 产品价格： | ￥900.0 |
| 规格： | 100mg | 产品价格： | ￥1210.0 |
| 规格： | 200mg | 产品价格： | ￥1596.0 |
| 基本信息 | |
| CAS | No.74711-43-6 |
| 中文名称 | 扎托布洛芬 |
| 英文名称 | Zaltoprofen |
| 别名 | CN100 |
| 分子式 | C17H14O3S |
| 分子量 | 298.36 |
| 溶解性 | Soluble in DMSO ≥5mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00864323 |
| SMILES | CC(C1=CC2=C(C=C1)SC3=CC=CC=C3C(=O)C2)C(=O)O |
| InChIKey | MUXFZBHBYYYLTH-UHFFFAOYSA-N |
| InChI | InChI=1S/C17H14O3S/c1-10(17(19)20)11-6-7-15-12(8-11)9-14(18)13-4-2-3-5-16(13)21-15/h2-8，10H，9H2，1H3，(H，19，20) |
| PubChem CID | 5720 |
| 靶点 | COX-2 |
| 通路 | Immunology & Inflammation |
| 背景说明 | 是一种COX-2抑制剂,对COX-1也有抑制作用，具有抗炎活性和对炎性疼痛的止痛作用。 |
| 生物活性 | Zaltoprofen 是一种具有优先口服活性的 COX-2 抑制剂，对 COX-1 和 COX-2 的 IC50 值分别为 1.3 和 0.34 μM。是一种非甾体抗炎药（NSAID），具有强大的抗炎作用，并对炎性疼痛有镇痛作用。[1-3] |
| IC50 | COX-1: 1.3μM(IC50);COX-2: 0.34μM(IC50) [1] |
| In Vitro | Mean IC50 values(microM)for human platelet cyclooxygenase-1 and interleukin-1beta-stimulated human synovial cell cyclooxygenase-2 and cyclooxygenase-1/-2 IC50 ratio of zaltoprofen was 1.3，0.34，3.8.[1] The above results suggest that zaltoprofen produces an analgesic action on bradykinin-induced nociceptive responses by blocking the B(2)receptor-mediated pathway in the primary sensory neurons. Zaltoprofen did not bind to B(1)and B(2)receptors in a radio-ligand binding assay. In the cultured dorsal root ganglion cells of mature mice，zaltoprofen completely inhibited the bradykinin-induced increase of [Ca(2+)](i). In addition，the inhibition of zaltoprofen on the increase of [Ca(2+)](i)was observed even under extracellular Ca(2+)-free conditions.[2] |
| 细胞实验 | With bradykinin-induced pain responses，CN-100 proved to be the most potent of the commercial non-steroidal antiinflammatory drugs which were tested in rats: The potency of CN-100 was 4 times stronger than that of indometacin. In mice，CN-100 was found to be as active as indometacin against peritonitis induced by acetic acid and pain responses induced by mechanical stimulus(pressure). Against the peritonitis induced by acetylcholine and phenyl-quinone，CN-100 showed inhibitory actions and its potencies were much stronger than those of aminophenazone(amino-pyrine)in mice.[3] |
| 数据来源文献 | [1]. Kawai S，et al. Comparison of cyclooxygenase-1 and -2 inhibitory activities of various nonsteroidal anti-inflammatory drugs using human platelets and synovial cells. Eur J Pharmacol. 1998 Apr 17;347(1):87-94. [2]. Hirate K，et al. Zaltoprofen，a non-steroidal anti-inflammatory drug，inhibits bradykinin-induced pain responses without blocking bradykinin receptors. Neurosci Res. 2006 Apr;54(4):288-94. [3]. Kameyama T，et al. Analgesic and antiinflammatory effects of 2-(10，11-dihydro-10-oxo-dibenzo[b，f]thiepin-2-yl)propionic acid in rat and mouse. Arzneimittelforschung. 1987 Jan;37(1):19-26. |
| 单位 | 瓶 |
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