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108427-72-1

中文名稱 108427-72-1
英文名稱 AS 35
CAS 108427-72-1
分子式 C21H20N6O4
分子量 420.42
MOL 文件 108427-72-1.mol
108427-72-1 結(jié)構(gòu)式 108427-72-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T14326
英文別名
AS 35
4H-Pyrido[1,2-a]pyrimidin-4-one, 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)-
3-(1H-Tetrazol-5-yl)-9-[[[2-propyl-3-hydroxy-4-(methylcarbonyl)phenyl]oxy]methyl]-4H-pyrido[1,2-a]pyrimidin-4-one

物理化學(xué)性質(zhì)

熔點(diǎn)269-271 °C
沸點(diǎn)678.8±65.0 °C(Predicted)
密度1.46±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)3?+-.0.10(Predicted)

常見問題列表

生物活性
AS-35 是一種有效的,可口服的,選擇性的 leukotrienes 拮抗劑,抑制 LTC4,LTD4 和 LTE4 誘導(dǎo)的回腸收縮, IC50 值分別為 8 nM,4 nM 和 3 nM,具有抗過敏的功效。
靶點(diǎn)

LTE 4

3 nM (IC 50 , In isolated guinea pig ileum)

LTD 4

4 nM (IC 50 , In isolated guinea pig ileum)

LTC 4

8 nM (IC 50 , In isolated guinea pig ileum)

體外研究

In isolated guinea pig preparations, AS-35 antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC 50 values of 8 nM, 4 nM and 3 nM, respectively. In the trachea, the agent also antagonizes LTD4 and LTE4-induced con tractions with IC 50 values of 10 nM and 20 nM, respectively. However, AS-35 does not antagonize LTC4-induced tracheal contraction in the presence of L-serine borate.

體內(nèi)研究

AS-35 (0.0375 to 0.3 mg/kg, i.v.) dose-dependently antagonizes bronchoconstriction induced by i.v.-injection of LTC4 and LTD4 in anesthetized guinea pigs, but does not inhibit histamine-induced bronchoconstriction. Oral administration of AS-35 also antagonizes LTD4 as well as antigen-induced LT-mediated bronchoconstriction. AS-35 (p.o.) inhibits LTD4-induced increase in the cutaneous vascular permeability of guinea pig.

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