Pregnenolone Carbonitrile
(Synonyms: 5-孕烷-3Β-醇-20-酮-16Α-腈,PCN,Pregnenolone 16α-carbonitrile,SC-4674) 目录号 : GC17893A rodent PXR agonist
Cas No.:1434-54-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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]。
References:
[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.
| Cas No. | 1434-54-4 | SDF | |
| 别名 | 5-孕烷-3Β-醇-20-酮-16Α-腈,PCN,Pregnenolone 16α-carbonitrile,SC-4674 | ||
| 化学名 | 3β-hydroxy-20-oxo-pregn-5-ene-16α-carbonitrile | ||
| Canonical SMILES | O[C@H](C1)CC[C@@]2(C)C1=CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])C[C@@H](C#N)[C@@H]4C(C)=O | ||
| 分子式 | C22H31NO2 | 分子量 | 341.5 |
| 溶解度 | ≤1mg/ml in ethanol;1mg/ml in methanol;1mg/ml in acetonitrile; 10mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9283 mL | 14.6413 mL | 29.2826 mL |
| 5 mM | 0.5857 mL | 2.9283 mL | 5.8565 mL |
| 10 mM | 0.2928 mL | 1.4641 mL | 2.9283 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。