Pregnenolone Carbonitrile

A rodent PXR agonist

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货号: ajci20028
CAS: 1434-54-4
别名: 5-孕烷-3Β-醇-20-酮-16Α-腈,PCN,Pregnenolone 16α-carbonitrile,SC-4674
分子式: C22H31NO2
分子量: 341.5
纯度: >98%
溶解度: ≤1mg/ml in ethanol;1mg/ml in methanol;1mg/ml in acetonitrile
储存: Store at -20°C
库存: 现货

Background

Pregnenolone-16α-carbonitrile is a rodent pregnane X receptor (PXR) activator involved in inducing the synthesis of a unique cytochrome P450 peptide in hepatic microsomes of male rats [1].

The nuclear pregnane X receptor (PXR) is an important component of the body’s adaptive defense mechanism against toxic substances. PXR could be activated by a large number of endogenous and exogenous chemicals such as antibiotics, steroids, antimycotics, and bile acids. PXR acts as a generalized sensor of hydrophobic toxins. PXR heterodimer binds with the 9-cis retinoic acid receptor (NR2B) to DNA response elements in the regulatory regions of cytochrome P450 3A monooxygenase genes and a number of other genes involved in the metabolism and elimination of xenobiotics from the body [2].

In vitro: In rat HSCs, PCN inhibited the trans-differentiation of rat HSCs in vitro despite the absence of PXR expression [3].

In vivo: PCN administration (25 mg/kg; one injection/week) to rats significantly increased the relative liver weight. In rats, PCN administration did not result in liver damage or significantly affect the level of liver damage caused by carbon tetrachloride. PCN treatment to carbon tetrachloride-treated rats resulted in a significant decrease in both intralobular α-smooth-muscle-actin immunostaining and intense Sirius Red staining in liver sections. PCN didn’t interfere with the metabolism of carbon tetrachloride to toxic metabolites [3].

孕酮-16α-碳腈是啮齿动物孕烷X受体（PXR）激活剂，参与诱导雄性大鼠肝微粒体中一种独特的细胞色素P450肽的合成[1]。

核孕烷X受体（PXR）是人体对有毒物质的适应性防御机制的重要组成部分。PXR可被内源性和外源性化学物质如抗生素、类固醇、抗真菌药物和胆汁酸等大量物质激活。PXR充当了亲水性毒素的广义传感器。PXR异二聚体与9-顺式视黄醛受体（NR2B）结合到细胞色素P450 3A单加氧酶基因的调节区和其他与代谢和清除体内外源性化学物质有关的基因的DNA反应元件[2]。

体外：在大鼠HSCs中，尽管没有PXR表达，PCN仍可抑制大鼠HSCs的转分化[3]。

体内：将PCN注射（25 mg/kg；每周一次）到大鼠体内显著增加了肝脏相对重量。在大鼠中，PCN的使用不会导致肝损伤，也不会显著影响四氯化碳引起的肝损伤水平。对四氯化碳处理后的大鼠进行PCN处理可导致肝脏组织中内叶α-平滑肌肌动蛋白免疫染色和Sirius Red染色明显降低。PCN不会干扰四氯化碳代谢产生的有毒代谢产物[3]。

参考文献:
[1] Birnbaum L S, Baird M B, Massie H R.? Pregnenolone-16alpha-carbonitrile-inducible cytochrome P450 in rat liver[J]. Research communications in chemical pathology and pharmacology, 1976, 15(3): 553.
[2] Kliewer S A, Goodwin B, Willson T M.? The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism[J]. Endocrine reviews, 2002, 23(5): 687-702.
[3] Marek C J, Tucker S J, Konstantinou D K, et al.? Pregnenolone-16α-carbonitrile inhibits rodent liver fibrogenesis via PXR (pregnane X receptor)-dependent and PXR-independent mechanisms[J]. Biochemical Journal, 2005, 387(3): 601-608.