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251992-66-2生产厂家

251992-66-2价格

251992-66-2

251992-66-2结构式
251992-66-2结构式

化源商城直购

中文名 4-[(4-甲基苯基)硫基]噻吩并[2,3-C]吡啶-2-甲酰胺
英文名 4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide
英文别名 Thieno[2,3-c]pyridine-2-carboxamide, 4-[(4-methylphenyl)thio]-
hms3269o07
4-[(4-Methylphenyl)sulfanyl]thieno[2,3-c]pyridine-2-carboxamide
unii-tp7tb1sszd
描述 A-205804 是抑制 E-selectin 和 ICAM-1 表达的口服有效的,高效、选择性的先导抑制剂,对 E-selectin 和 ICAM-1 作用的 IC50 分别为 20 nM 和 25 nM。A-205804 可用于慢性炎症疾病的研究。
相关类别
靶点

IC50: 20 nM (E-selectin), 25 nM (ICAM-1)[1]

体外研究 A-205804对HUVEC有细胞毒性,IC50为152μM[1]。在体外流动实验中,A-205804是一种有效的细胞-细胞粘附抑制剂,在模型生理系统中显示出相关性[1]。
体内研究 A-205804(5 mg/kg;p.o.)显示大鼠的半衰期为1小时[1]。A-205804(10 mg/kg;p.o.;每周3次;持续2周)减弱小鼠内皮血管龛细胞上E-选择素的表达[2]。动物模型:C57BL/6小鼠[2]剂量:10mg/kg给药:口服,每周3次,连续2周结果:有效降低内皮血管龛细胞E-选择素的表达动物模型:大鼠[1]剂量:5mg/kg给药:口服结果:t1/2=1小时
参考文献

[1]. Stewart AO, et al. Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression. J Med Chem. 2001 Mar 15;44(6):988-1002.

[2]. Morita K, et al. RUNX transcription factors potentially control E-selectin expression in the bone marrow vascular niche in mice. Blood Adv. 2018 Mar 13;2(5):509-515.

密度 1.4±0.1 g/cm3
沸点 581.3±45.0 °C at 760 mmHg
熔点 198-199℃
分子式 C15H12N2OS2
分子量 300.399
闪点 305.4±28.7 °C
精确质量 300.039093
PSA 109.52000
LogP 3.07
外观性状 固体;White to Orange to Green powder to crystal
蒸汽压 0.0±1.6 mmHg at 25°C
折射率 1.738
储存条件 Store at +4°C
危害码 (欧洲) Xi

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251992-66-2结构式

251992-66-2

文献:Abbott Laboratories Patent: US6232320 B1, 2001 ;

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251992-66-2结构式

251992-66-2

文献:Stewart; Bhatia; McCarty; Patel; Staeger; Arendsen; Gunawardana; Melcher; Zhu; Boyd; Fry; Cool; Kiflie; Lartey; Marsh; Kempf-Grote; Kilgannon; Wisdom; Meyer; Gallatin; Okasinskit Journal of Medicinal Chemistry, 2001 , vol. 44, # 6 p. 988 - 1002

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251992-66-2结构式

251992-66-2

文献:Stewart; Bhatia; McCarty; Patel; Staeger; Arendsen; Gunawardana; Melcher; Zhu; Boyd; Fry; Cool; Kiflie; Lartey; Marsh; Kempf-Grote; Kilgannon; Wisdom; Meyer; Gallatin; Okasinskit Journal of Medicinal Chemistry, 2001 , vol. 44, # 6 p. 988 - 1002

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251992-66-2结构式

251992-66-2

文献:Stewart; Bhatia; McCarty; Patel; Staeger; Arendsen; Gunawardana; Melcher; Zhu; Boyd; Fry; Cool; Kiflie; Lartey; Marsh; Kempf-Grote; Kilgannon; Wisdom; Meyer; Gallatin; Okasinskit Journal of Medicinal Chemistry, 2001 , vol. 44, # 6 p. 988 - 1002

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251992-66-2结构式

251992-66-2

文献:Stewart; Bhatia; McCarty; Patel; Staeger; Arendsen; Gunawardana; Melcher; Zhu; Boyd; Fry; Cool; Kiflie; Lartey; Marsh; Kempf-Grote; Kilgannon; Wisdom; Meyer; Gallatin; Okasinskit Journal of Medicinal Chemistry, 2001 , vol. 44, # 6 p. 988 - 1002
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