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327610-87-7

中文名稱 327610-87-7
英文名稱 NO-prednisolone
CAS 327610-87-7
分子式 C29H33NO9
分子量 539.57
MOL 文件 327610-87-7.mol
327610-87-7 結(jié)構(gòu)式 327610-87-7 結(jié)構(gòu)式

基本信息

中文別名
NO-潑尼松龍
英文別名
NCX-1015
NO-prednisolone
Pregna-1,4-diene-3,20-dione, 11,17-dihydroxy-21-[[4-[(nitrooxy)methyl]benzoyl]oxy]-, (11β)-
[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] 4-(nitrooxymethyl)benzoate

物理化學(xué)性質(zhì)

沸點(diǎn)736.2±60.0 °C(Predicted)
密度1.39±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)12.30±0.70(Predicted)
形態(tài)Solid
顏色White to yellow

常見(jiàn)問(wèn)題列表

生物活性
NO-prednisolone 是釋放一氧化氮 (NO) 的 Prednisolone 衍生物。NO-prednisolone 有效刺激體內(nèi) IL-10 產(chǎn)生。
靶點(diǎn)

IL-10

體外研究

NO-prednisolone (NCX-1015), an NO-releasing derivative of Prednisolone, is demonstrated to be more effective than Prednisolone in reducing inflammation, inhibiting cytokine and chemokine generation, and up-regulating the expression of the steroid-sensitive cell-surface marker CD163 in human peripheral blood mononuclear cells Incubation of PBMCs with NO-prednisolone (NCX-1015) and Prednisolone produces a concentration-dependent activation of CD163. NO-prednisolone is more potent than Prednisolone at inducing CD163 cell surface expression. The increased efficacy of NO-prednisolone, compared with the parent molecule Prednisolone, is also observed when assessing inhibition of LPS induced IL-1β production.

體內(nèi)研究

In vivo treatment with NO-prednisolone (NCX-1015) potently stimulates IL-10 production, suggesting that the NO steroid induces a regulatory subset of T cells that negatively modulates intestinal inflammation. The two doses of NO-prednisolone tested, 0.5 and 5 mg/kg/day (equivalent to 0.33 and 3.3 mg/kg/day prednisone, respectively) effectively attenuates the severity of the wasting syndrome, ameliorates the colitis score, and reduces the colonic myeloperoxidase (MPO) activity. NO-prednisolone administration also reduces the colonic mRNA and protein content of tumor necrosis factor-α, IL-12, and IFN-γ. NO-prednisolone also reduces the expression of inducible NO synthase and cyclooxygenase-2 but in contrast does not inhibit colonic expression of IL-10 mRNA or protein. In fact, IL-10 expression is enhanced in mice treated with NO-prednisolone.

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