2. Membrane Transporter/Ion Channel Neuronal Signaling NF-κB Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Immunology/Inflammation
  3. Calcium Channel NF-κB Pregnane X Receptor (PXR) Cytochrome P450 Interleukin Related
  4. Praeruptorin E

Praeruptorin E is an orally active pyranocoumarin compound. Praeruptorin E can be isolated from the dried roots of Peucedanum praeruptorum Dunn. Praeruptorin E reduces the expression of NF-κB. Praeruptorin E upregulates the expression of PXR and CYP3A4. Praeruptorin E inhibits Th2 cytokines, TNF-α, IL6, MPO, and blocks the Ca2+ slow channel. Praeruptorin E promotes pulmonary tissue repair and relaxes porcine coronary artery strips. Praeruptorin E protects mice from lipopolysaccharide- and hydrochloric acid-induced acute lung injury. Praeruptorin E can be used in studies related to asthma and acute lung injury.

For research use only. We do not sell to patients.

Praeruptorin E

Praeruptorin E Chemical Structure

CAS No. : 78478-28-1

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Other Forms of Praeruptorin E:

Praeruptorin E Related Antibodies

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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  • Purity & Documentation

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  • Customer Review

Description

Praeruptorin E is an orally active pyranocoumarin compound. Praeruptorin E can be isolated from the dried roots of Peucedanum praeruptorum Dunn. Praeruptorin E reduces the expression of NF-κB. Praeruptorin E upregulates the expression of PXR and CYP3A4. Praeruptorin E inhibits Th2 cytokines, TNF-α, IL6, MPO, and blocks the Ca2+ slow channel. Praeruptorin E promotes pulmonary tissue repair and relaxes porcine coronary artery strips. Praeruptorin E protects mice from lipopolysaccharide- and hydrochloric acid-induced acute lung injury. Praeruptorin E can be used in studies related to asthma and acute lung injury[1][2][3].

IC50 & Target[1][2]

CYP3A4

 

IL-6

 

In Vitro

Praeruptorin E (60 μM; 24 h) reduces NF-κB p65 expression and increases PXR and CYP3A4 expression in LPS-induced human L-02 fetal hepatocytes, and this effect is partially dependent on PXR expression[1].
Praeruptorin E (60 μM) reduces the binding of NF-κB p65 to the PXR gene promoter in human L-02 fetal hepatocytes, as evidenced by a significant decrease in NF-κB enrichment at this region[1].
Praeruptorin E (4.7 μM) acts as a calcium antagonist on potassium-depolarized swine coronary artery strips with a pD2' value of 5.2, inhibiting Ca2+-induced maximum contraction and shifting the Ca2+ concentration-response curve rightward in a non-parallel manner[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Praeruptorin E Related Antibodies
In Vivo

Praeruptorin E (administered via gavage; once daily for 7 consecutive days at doses of 2.5-40 mg/kg) enhances the anti-asthmatic effect of Aminophylline (HY-B0140) on Ovalbumin (HY-W250978)-induced asthmatic mice by alleviating airway inflammation, mucus secretion and collagen deposition, while also reducing Aminophylline-induced cardiotoxicity, with the 40 mg/kg dose exerting the strongest effect[1].
Praeruptorin E (20-80 mg/kg; p.o.; single administration 1 hour prior to LPS challenge) dose-dependently attenuates LPS-induced acute lung injury in male BALB/c mice. At the dose of 80 mg/kg, it inhibits neutrophil (PMNs) infiltration by 53%, TNF-α release by 56%, and IL-6 release by 51%, while also suppressing the activation of the NF-κB pathway and ameliorating histopathological changes in lung tissue[2].
Praeruptorin E (80 mg/kg; p.o.; single administration 1 h prior to hydrochloric acid challenge) protects male BALB/c mice against hydrochloric acid-induced acute lung injury by reducing polymorphonuclear neutrophil (PMNs) infiltration, IL-6 release, protein extravasation and pulmonary histopathological damage[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (male, 18-22 g, ovalbumin-induced asthma)[1]
Dosage: 2.5 mg/kg; 10 mg/kg; 40 mg/kg
Administration: i.g.; daily; 7 days
Result: Significantly reduced total inflammatory cells, eosinophils, monocytes, neutrophils, and lymphocytes in bronchoalveolar lavage fluid compared to aminophylline alone, with the 40 mg/kg dose showing the greatest reduction.
Significantly lowered lung and bronchial histopathological scores compared to aminophylline alone, with the 40 mg/kg dose showing the least severe pathological changes including reduced inflammatory cell infiltration, alveolar wall thickening, and bronchial mucosal edema.
Significantly reduced mucus secretion (PAS-positive area) and collagen deposition (fibrosis area) in lung tissue compared to aminophylline alone, with the 40 mg/kg dose showing the largest reduction.
Significantly lowered concentrations of BALF IL-4, IL-5, IL-13, serum IgE, and NF-κB p65 compared to aminophylline alone.
Significantly reduced lung tissue NF-κB p65 protein and mRNA expression compared to aminophylline alone, while significantly increased liver tissue PXR and CYP3A11 protein and mRNA expression compared to aminophylline alone.
Showed no significant differences in CYP1A2 and CYP2E1 expression across groups.
Improved heart rhythm regularity, reduced premature ventricular beats, and significantly lowered serum LDH and CK-MB levels compared to aminophylline alone when combined with a high (cardiotoxic) dose of aminophylline (450 mg/kg).
Animal Model: BALB/c (male, 6-8 weeks old, 20-25 g, LPS-induced acute lung injury)[2]
Dosage: 20 mg/kg; 40 mg/kg; 80 mg/kg
Administration: p.o.; single dose 1 hour before LPS challenge
Result: Reduced bronchoalveolar lavage fluid total cell counts from 792×103/mL to 472×103/mL at 80 mg/kg.
Reduced bronchoalveolar lavage fluid PMNs counts from 648×103/mL to 381×103/mL at 80 mg/kg.
Reduced bronchoalveolar lavage fluid TNF-α levels from 6.645 ng/mL to 3.962 ng/mL at 80 mg/kg.
Reduced bronchoalveolar lavage fluid IL-6 levels from 1.096 ng/mL to 0.523 ng/mL at 80 mg/kg.
Caused 11%, 43%, and 53% inhibition of LPS-induced PMNs counts at 20 mg/kg, 40 mg/kg, and 80 mg/kg, respectively.
Achieved 56% inhibition of TNF-α levels and 51% inhibition of IL-6 levels at 80 mg/kg.
Reduced LPS-induced protein extravasation in bronchoalveolar lavage fluid in a dose-dependent manner.
Reduced lung myeloperoxidase (MPO) activity at 80 mg/kg.
Attenuated LPS-induced lung pathological changes including neutrophil infiltration, alveolar wall swelling, hemorrhage, and alveolar structural damage at 80 mg/kg.
Inhibited LPS-induced cytoplasmic loss of IκB-α protein at 80 mg/kg.
Suppressed translocation of NF-κB p65 from cytoplasm to nucleus at 80 mg/kg.
Animal Model: BALB/c (male, 6-8 weeks old, 20-25 g, HCl-induced acute lung injury)[2]
Dosage: 80 mg/kg
Administration: p.o.; single dose 1 hour before HCl challenge
Result: Reduced HCl-induced PMNs counts in bronchoalveolar lavage fluid.
Decreased HCl-induced IL-6 levels in bronchoalveolar lavage fluid.
Inhibited HCl-induced protein extravasation in bronchoalveolar lavage fluid.
Attenuated HCl-induced lung pathological changes including severe hemorrhage, neutrophil infiltration, and alveolar structural damage.
Molecular Weight

428.47

Formula

C24H28O7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)CC(O[C@H]1C2=C(OC(C)(C)[C@H]1OC(/C(C)=C\C)=O)C=CC(C=C3)=C2OC3=O)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (58.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3339 mL 11.6694 mL 23.3389 mL
5 mM 0.4668 mL 2.3339 mL 4.6678 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3339 mL 11.6694 mL 23.3389 mL 58.3471 mL
5 mM 0.4668 mL 2.3339 mL 4.6678 mL 11.6694 mL
10 mM 0.2334 mL 1.1669 mL 2.3339 mL 5.8347 mL
15 mM 0.1556 mL 0.7780 mL 1.5559 mL 3.8898 mL
20 mM 0.1167 mL 0.5835 mL 1.1669 mL 2.9174 mL
25 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3339 mL
30 mM 0.0778 mL 0.3890 mL 0.7780 mL 1.9449 mL
40 mM 0.0583 mL 0.2917 mL 0.5835 mL 1.4587 mL
50 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1669 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Praeruptorin E78478-28-1Calcium ChannelNF-κBPregnane X Receptor (PXR)Cytochrome P450Interleukin RelatedCa2+ channelsCa channelsNuclear factor-κBNuclear factor-kappaBPregnane X ReceptorCYPsILTh2 cytokineshuman L-02 fetal hepatocytesTNF-αIκB-αIL-6p65CYP3A4BALB/c micePXRInhibitorinhibitorinhibit

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