Periplogenin
Based on 1 publication(s) in Google Scholar
Periplogenin is an orally active cardiac glycoside found in Cortex periplocae. Periplogenin can induce ROS production and necroptosis and cause G0/G1 phase arrest. Periplogenin can inhibit pyroptosis by regulating the NLRP3/Caspase-1/GSDMD signaling. Periplogenin suppresses growth of prostate carcinoma cells by docking to an ATP1A1 protein pocket and forming a hydrogen bond with T804. Periplogenin can be used for the researches of cancer, inflammation and immunology, such as prostate carcinoma, rheumatoid arthritis and psoriasis.
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- Pureza: 99.34%
- No. CAS: 514-39-6
- Fòrmula: C23H34O5
- Peso molecular:390.51
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Periplogenin
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
Ver todos los productos específicos de isoformas Caspase
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Actividad biológica
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IL-1β |
IL-18 |
Caspase-1 |
NLRP3 |
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Cell Line
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Type | Value | Description | References |
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| HT-1080 | IC50 |
810 nM
Compound: 11
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Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay
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[PMID: 14640513] |
Periplogenin (0.625-10 μg/mL 44 h) inhibits the viability of human HaCaT keratinocytes, with an IC50 of 1.56 μg/mL[1].
Periplogenin (2 μg/mL, 6-24 h) induces caspase-independent non-apoptotic and non-autophagic cell death in HaCaT cells[1].
Periplogenin (1-4 μg/mL, 12-48 h) increases ROS production and induces necroptosis in HaCaT cells[1].
Periplogenin (0.1-20 μg/mL, 24 h) inhibits the proliferation of rheumatoid arthritis fibroblast-like synoviocytes (RA-FLS), with an IC50 of 1.56 μg/mL[2].
Periplogenin (0.1-5 μg/mL, 24 h) inhibits the migration, invasion and pyroptosis in RA-FLS[2].
Periplogenin (0.1-5 μg/mL, 24 h) induces G0/G1 phase arrest in RA-FLS[2].
Periplogenin (0.1-5 μg/mL, 24 h) downregulates NLRP3, Cleaved-Caspase-1, GSDMD-N, IL-1β, and IL-18 expression in RA-FLS[2].
Periplogenin (0.02-33 μM, 72 h) inhibits the viability of DU145, DLD-1, U-87MG, and MCF-7 cancer cells, with IC50 values of 2.897 μM, 8.712 μM, 3.008 μM, and 20.025 μM respectively[3].
Periplogenin (0-100 μM) inhibits the enzymatic activity of ATP1A1 in wild-type DU145 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT cells
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Concentration:1, 2 and 4 μg/mL
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Incubation Time:24 and 48 h
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Result:Disrupted the membrane integrity.
Increased PI uptake and LDH release.
Revealed necrotic features (cytoplasmic swelling, reduced organelles, nuclear membrane disorder).
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Cell Line:RA-FLS
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Concentration:0.1, 0.5 and 5 μg/mL
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Incubation Time:24 h
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Result:Increased the proportion of G0/G1 phase cells.
Decreased the proportion of G2/M phase cells.
Showed no significant change in S phase cell proportion.
Periplogenin (10-20 mg/kg, i.g., once a day) inhibits tumor growth in DU145 wild-type xenograft mice models[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TPA-induced and IMQ (HY-B0180)-induced psoriasis-like mice models[1]
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Dosage:2 μg per site
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Administration:Topical application, daily for 11 days starting after 8 days of TPA induction
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Result:Reduced ear thickness and weight.
Alleviated epidermal hyperplasia and inflammatory cell infiltration in dorsal skin and ears.
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Animal Model:DU145 wild-type xenograft mice models[3]
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Dosage:10 and 20 mg/kg
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Administration:Orally gavage, once a day
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Result:Reduced tumor volume and weight.
Had no significant change in body weight.
Chemical Information
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No. CAS 514-39-6
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Appearance Solid
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Peso molecular 390.51
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Fòrmula C23H34O5
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Color White to off-white
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SMILES
O[C@@]12[C@@]3([H])[C@@](CC[C@@]1([C@@H](C4=CC(OC4)=O)CC2)C)([H])[C@@]5([C@@](O)(C[C@@H](O)CC5)CC3)C
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Periplogenin inhibits pyroptosis of fibroblastic synoviocytes in rheumatoid arthritis through the NLRP3/Caspase-1/GSDMD signaling pathway. [Abstract]2024 May 30:133:112041. PMID: 38636373
Periplogenin purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 May 30:133:112041. [Abstract]
Effect of Periplogenin PPN on the cell proliferation of RA-FLS.
Periplogenin purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 May 30:133:112041. [Abstract]
Cell wound healing in the scratch test for 24 h treated with Periplogenin (PPN) (0.1, 0.5, 5 μg/mL).
Periplogenin purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 May 30:133:112041. [Abstract]
Transwell test cell invasion ability treated with Periplogenin (PPN) (0.1, 0.5, 5 μg/mL).
Periplogenin purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 May 30:133:112041. [Abstract]
Pyroptosis was determined by flow cytometry treated with Periplogenin (PPN) (0.1, 0.5, 5 μg/mL).
Periplogenin purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 May 30:133:112041. [Abstract]
Relative expression of NLRP3, GSDMD, Caspase-1, IL-1β, IL-18 treated with Periplogenin (PPN) (0.1, 0.5, 5 μg/mL).
Solvente y solubilidad
DMSO : 100 mg/mL (256.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (286 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zhang WJ, et al. Periplogenin induces necroptotic cell death through oxidative stress in HaCaT cells and ameliorates skin lesions in the TPA- and IMQ-induced psoriasis-like mouse models. Biochem Pharmacol. 2016 Apr 1;105:66-79. [Content Brief]
[2]. Ma X, et al. Periplogenin inhibits pyroptosis of fibroblastic synoviocytes in rheumatoid arthritis through the NLRP3/Caspase-1/GSDMD signaling pathway. Int Immunopharmacol. 2024 May 30;133:112041. [Content Brief]
[3]. Zhang X, et al. The natural compound periplogenin suppresses the growth of prostate carcinoma cells by directly targeting ATP1A1. Sci Rep. 2024 Sep 3;14(1):20509. [Content Brief]
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 | 2.5608 mL | 12.8038 mL | 25.6075 mL | 64.0188 mL |
| 5 mM | 0.5122 mL | 2.5608 mL | 5.1215 mL | 12.8038 mL | |
| 10 mM | 0.2561 mL | 1.2804 mL | 2.5608 mL | 6.4019 mL | |
| 15 mM | 0.1707 mL | 0.8536 mL | 1.7072 mL | 4.2679 mL | |
| 20 mM | 0.1280 mL | 0.6402 mL | 1.2804 mL | 3.2009 mL | |
| 25 mM | 0.1024 mL | 0.5122 mL | 1.0243 mL | 2.5608 mL | |
| 30 mM | 0.0854 mL | 0.4268 mL | 0.8536 mL | 2.1340 mL | |
| 40 mM | 0.0640 mL | 0.3201 mL | 0.6402 mL | 1.6005 mL | |
| 50 mM | 0.0512 mL | 0.2561 mL | 0.5122 mL | 1.2804 mL | |
| 60 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0670 mL | |
| 80 mM | 0.0320 mL | 0.1600 mL | 0.3201 mL | 0.8002 mL | |
| 100 mM | 0.0256 mL | 0.1280 mL | 0.2561 mL | 0.6402 mL |
Periplogenin Related Classifications
HY-N2414 Related Classifications
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