| Bioactivity | Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults[1][2][3]. | |||||||||
| Invitro | Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults[1][2][3]. | |||||||||
| In Vivo | Pregnenolone 16α-carbonitrile (40 mg/kg/day; i.p.; for two days) induces the expression of Cyp3a11 and Cyp2b10 at the mRNA, protein, and enzymatic levels in WT mice[1]. Pregnenolone 16α-carbonitrile (100 mg/kg; ip; single dose) induces the expression of CYP3A mRNA in adult female Sprague-Dawley rats weighing 150-200 g[2]. Pregnenolone 16α-carbonitrile (35 mg/kg; gavage; once daily for three days) increase in Pgp expression in male Sprague-Dawley rats, aged approximately 100 days and weighing 250-400 g[3]. Animal Model: | |||||||||
| Name | Pregnenolone 16α-carbonitrile | |||||||||
| CAS | 1434-54-4 | |||||||||
| Formula | C22H31NO2 | |||||||||
| Molar Mass | 341.49 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. |