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5-孕烷-3β-醇-20-酮-16Alpha-腈

5-孕烷-3β-醇-20-酮-16Alpha-腈用途

孕烯醇酮16α-碳腈是一种口服活性的原型和有效的啮齿动物PXR激活剂。孕烯醇酮16α-碳腈是一种合成类固醇,可诱导细胞色素P4503A的表达。孕烯醇酮16α-碳腈对随后的应激性侮辱表现出更强的抵抗力[1][2][3]。

5-孕烷-3β-醇-20-酮-16Alpha-腈名称

[ CAS 号 ]:
1434-54-4

[ 中文名 ]:
5-孕烷-3β-醇-20-酮-16Alpha-腈

[ 英文名 ]:
Pregnenolone 16α-carbonitrile

[中文别名 ]:

5-孕烷-3Β-醇-20-酮-16Α-腈

[英文别名 ]:

MFCD00079212
16 α-Carbonitrile, Pregnenolone
pregnenolone 16alpha-carbonitrile
pregnenolone carbonitrile
Pregnenolone 16α-carbonitrile
Pregnenolone-16alpha-carbonitrile
5-Pregnen-3beta-ol-20-one-16alpha-carbonitrile

5-孕烷-3β-醇-20-酮-16Alpha-腈生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450

研究领域 >> 代谢疾病

[体外研究]

孕烯醇酮16α-碳腈(20μM；9天)直接抑制大鼠肝星状细胞(HSC)转分化为促纤维化表型,尽管细胞不表达PXR(与肝细胞相比)[4]。

[体内研究]

孕烯醇酮16α-碳腈(40 mg/kg/天；静脉注射；持续两天)在WT小鼠的mRNA、蛋白质和酶水平诱导Cyp3a11和Cyp2b10的表达[1]。孕烯醇酮16α-碳腈(100 mg/kg；ip；单剂量)诱导体重150-200 g的成年雌性Sprague-Dawley大鼠CYP3A mRNA的表达[2]。孕烯醇酮16α-碳腈(35 mg/kg；灌胃；每天一次,连续三天)增加雄性Sprague-Dawley大鼠的Pgp表达,年龄约为100天,体重250-400 g[3]。动物模型：WT和Pxr-/-小鼠[1]剂量：40mg/kg给药：IP；结果：诱导WT小鼠在mRNA、蛋白质和酶水平上表达Cyp3a11和Cyp2b10。对Pxr-/-小鼠Cyp3a11的表达几乎没有影响

[参考文献]

[1]. Yang Xie, et al. Activation of Pregnane X Receptor Sensitizes Mice to Hemorrhagic Shock-Induced Liver Injury. Hepatology. 2019 Sep;70(3):995-1010.

[2]. Simon Lowes, et al. The Effects of Pregnenolone 16α-Carbonitrile Dosing on Digoxin Pharmacokinetics and Intestinal Absorption in the Rat. Pharmaceutics. 2010 Mar 15;2(1):61-77.

[3]. Jeffrey Guzelian, et al. Identification of genes controlled by the pregnane X receptor by microarray analysis of mRNAs from pregnenolone 16alpha-carbonitrile-treated rats. Toxicol Sci. 2006 Dec;94(2):379-87.

[4]. Carylyn J Marek, et al. Pregnenolone-16alpha-carbonitrile inhibits rodent liver fibrogenesis via PXR (pregnane X receptor)-dependent and PXR-independent mechanisms. Biochem J. 2005 May 1;387(Pt 3):601-8.

5-孕烷-3β-醇-20-酮-16Alpha-腈物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
508.5±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₂H₃₁NO₂

[ 分子量 ]:
341.487

[ 闪点 ]:
261.3±30.1 °C

[ 精确质量 ]:
341.235474

[ PSA ]:
61.09000

[ LogP ]:
3.22

[ 蒸汽压 ]:
0.0±3.0 mmHg at 25°C

[ 折射率 ]:
1.558

[ 储存条件 ]:
-20°C，密闭，干燥

5-孕烷-3β-醇-20-酮-16Alpha-腈安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
TU4536500

5-孕烷-3β-醇-20-酮-16Alpha-腈合成路线

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5-孕烷-3β-醇-20-酮-16Alpha-腈文献

Pregnane X receptor agonists impair postprandial glucose tolerance.

Clin. Pharmacol. Ther. 93(6) , 556-63, (2013)

We conducted a randomized, open, placebo-controlled crossover trial to investigate the effects of the pregnane X receptor (PXR) agonist rifampin on an oral glucose tolerance test (OGTT) in 12 healthy ...

The cytochrome P450 2AA gene cluster in zebrafish (Danio rerio): expression of CYP2AA1 and CYP2AA2 and response to phenobarbital-type inducers.

Toxicol. Appl. Pharmacol. 272(1) , 172-9, (2013)

The cytochrome P450 (CYP) 2 gene family is the largest and most diverse CYP gene family in vertebrates. In zebrafish, we have identified 10 genes in a new subfamily, CYP2AA, which does not show orthol...

Decreased apoptosis during CAR-mediated hepatoprotection against lithocholic acid-induced liver injury in mice.

Toxicol. Lett. 188(1) , 38-44, (2009)

Myeloid cell leukemia-1 (Mcl-1) is an anti-apoptotic protein that is regulated by the constitutive androstane receptor (CAR). Activation of CAR can protect the liver against bile acid-induced toxicity...

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