Pregnenolone Carbonitrile (Synonyms: PCN,Pregnenolone 16α-carbonitrile,SC-4674) |
| Catalog No.GC17893 |
프레그네놀론 카보니트릴은 구강 투여가 가능한 원형이며, 유익한 쥐-PXR 활성화제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1434-54-4
Sample solution is provided at 25 µL, 10mM.
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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].
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 | |
| Synonyms | PCN,Pregnenolone 16α-carbonitrile,SC-4674 | ||
| Chemical Name | 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 | ||
| Formula | C22H31NO2 | M.Wt | 341.5 |
| Solubility | ≤1mg/ml in ethanol;1mg/ml in methanol;1mg/ml in acetonitrile; 10mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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