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101193-62-8

中文名稱 101193-62-8
英文名稱 FK-021
CAS 101193-62-8
分子式 C17H13N6NaO3
分子量 372.32
MOL 文件 101193-62-8.mol
101193-62-8 結構式 101193-62-8 結構式

基本信息

中文別名
喹托司特鈉
英文別名
FK-021
FR-71021
Quinotolast sodium
4-Oxo-1-phenoxy-N-(1-sodio-1H-tetrazol-5-yl)-4H-quinolizine-3-carboxamide

物理化學性質

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色Light yellow to yellow

常見問題列表

生物活性
Quinotolast sodium (濃度范圍為 1-100 μg/mL) 抑制組胺,LTC4 和 PGD2 釋放,這種作用具有濃度依賴性。
靶點

LTC 4

PGD 2

Histamine

體外研究

Quinotolast inhibits the release of histamine and the generation of leukotriene (LT) C 4 and prostaglandin (PG) D 2 from dispersed human lung cells. Quinotolast (100 μg/mL) significantly inhibits PGD 2 and LTC 4 release. Quinotolast inhibits PGD 2 release by 100% and LTC 4 release by 54%. The inhibitory effect of Quinotolast on histamine release from dispersed lung cells is largely independent of the preincubation period, no tachyphylaxis being observed. Quinotolast shows a significant inhibition of inflammatory mediators from human dispersed lung cells. Quinotolast also shows strong inhibitory effects on histamine and peptide leukotrienes release from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLTs release from cultured mast cells. The IC 50 value for Quinotolast is 0.72 μg/mL.

體內(nèi)研究

Quinotolast potently inhibits such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. When Quinotolast is given i.v. to rats, Quinotolast, dose-dependently inhibits PCA. The doses of Quinotolast required to inhibit the reaction by 50% (ED 50 ) is 0.0063 mg/kg. Given p.o., Quinotolast inhibits the reaction. ED 50 value for Quinotolast is 0.0081 mg/kg. Although almost complete inhibition is observed with Quinotolast at a dose of 0.32 mg/kg, its effect is slightly attenuated at a dose of 1 mg/kg.

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