Paxilline
Based on 10 publication(s) in Google Scholar
Paxilline is an indole alkaloid mycotoxin derived from Penicillium paxilli, which effectively inhibits the BK channel through a channel-blocking mechanism. Paxilline also inhibits sarco/endoplasmic reticulum Ca2+-stimulated ATPase (SERCA), with IC50 values ranging from 5 μM to 50 μM for different SERCA isoforms. Paxilline exhibits significant anticonvulsant and neuroprotective effects, as well as certain antioxidant activity.
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- Reinheit: 99.91%
- CAS. Nr.: 57186-25-1
- Formel: C27H33NO4
- Molecular Weight:435.56
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Paxilline
More- Nat Commun. 2023 Dec 12;14(1):8255. [Abstract]
- J Clin Invest. 2024 Jul 2:e176328. [Abstract]
- Appl Phys Rev. 2026 Jan 21.
- Biomed Pharmacother. 2022 Mar:147:112641. [Abstract]
- Mol Cells. 2021 Aug 31;44(8):557-568. [Abstract]
- Am J Physiol Cell Physiol. 2025 Oct 1;329(4):C1130-C1138. [Abstract]
- Cell Calcium. 2026 Mar:134:103117. [Abstract]
- Cell Calcium. 2022 Jun;104:102571. [Abstract]
- J Cell Physiol. 2021 Aug;236(8):5818-5831. [Abstract]
- bioRxiv. 2025 Sep 21.
Alle Calcium Channel Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| MDCK | IC50 |
17.7 μM
Compound: 10
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Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) PR/8 infected in MDCK cells assessed as protection against virus-induced cytopathogenicity after 48 hrs by crystal-violet staining-based assay
Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) PR/8 infected in MDCK cells assessed as protection against virus-induced cytopathogenicity after 48 hrs by crystal-violet staining-based assay
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[PMID: 23886345] |
Paxilline (1-4 μM, 18 h) exhibits a dose-dependent protective effect in HT22 cells, alleviating glutamate-induced neurotoxicity independently of BKCa channel inhibition[4]. axilline (1 μM, 3–48 h) partially alleviates Cd2+-induced necrosis and reduces ROS generation in PC12 and AS-30D cells but does not inhibit Cd2+-induced apoptosis or mitochondrial membrane potential decline. Paxilline may exert its protective effects through modulation of the mitochondrial electron transport chain[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Glutamate-induced cytotoxicity HT22 cell model (mouse hippocampal neuronal cells)
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Concentration:1, 2, 4 μM
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Incubation Time:18 hours
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Result:Increased cell survival in the 3 mM glutamate-induced cytotoxicity model, protecting HT22 cells from glutamate-induced cell death.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Thalidomide-induced cognitive impairment C57BL/6 mouse model[6]
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Dosage:3 μg/kg
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Administration:Intraperitoneal injection (i.p.), single dose (3 hours before behavioral tests)
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Result:Reversed Thalidomide-induced cognitive impairment, restoring memory function in the Passive Avoidance Test and Novel Object Recognition Test, improving working memory in the Y-Maze Test, and alleviating anxiety and depressive behaviors in the Elevated Plus Maze Test and Tail-Suspension Test.
Chemical Information
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CAS. Nr. 57186-25-1
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Appearance Solid
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Molecular Weight 435.56
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Formel C27H33NO4
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Color White to off-white
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SMILES
O=C1[C@@H](C(C)(O)C)O[C@](CC2)([H])C([C@]([C@@]2(C)[C@]34C)(O)CC[C@@]3([H])CC5=C4NC6=C5C=CC=C6)=C1
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Nat Commun
D-serine reconstitutes synaptic and intrinsic inhibitory control of pyramidal neurons in a neurodevelopmental mouse model for schizophrenia. [Abstract]2023 Dec 12;14(1):8255. PMID: 38086803 -
J Clin Invest
Potentiation of BKCa channels by cystic fibrosis transmembrane conductance regulator (CFTR) correctors VX-445 and VX-121. [Abstract]2024 Jul 2:e176328. PMID: 38954478 -
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Biomed Pharmacother
Protective role of activating PPARγ in advanced glycation end products-induced impairment of coronary artery vasodilation via inhibiting p38 phosphorylation and reactive oxygen species production. [Abstract]2022 Mar:147:112641. PMID: 35051861 -
Mol Cells
BK Channel Deficiency in Osteoblasts Reduces Bone Formation via the Wnt/β-Catenin Pathway. [Abstract]2021 Aug 31;44(8):557-568. PMID: 34385407 -
Am J Physiol Cell Physiol
(R)-vanzacaftor potentiates BKCa channels in the absence of CFTR correction or potentiation. [Abstract]2025 Oct 1;329(4):C1130-C1138. PMID: 40920663 -
Cell Calcium
2026 Mar:134:103117. PMID: 41539212 -
Cell Calcium
Mechanosensitive Piezo1 channel in rat epididymal epithelial cells promotes transepithelial K+ secretion. [Abstract]2022 Jun;104:102571. PMID: 35314382 -
J Cell Physiol
BKCa channel participates in insulin-induced lipid deposition in adipocytes by increasing intracellular calcium. [Abstract]2021 Aug;236(8):5818-5831. PMID: 33432604 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (229.59 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 6.25 mg/mL (14.35 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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 (5.74 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.
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.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Portuguese - PT (644 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Zhou Y, et al. Paxilline inhibits BK channels by an almost exclusively closed-channel block mechanism. J Gen Physiol. 2014 Nov;144(5):415-40. [Content Brief]
[2]. Bilmen JG, et al. The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline. Arch Biochem Biophys. 2002 Oct 1;406(1):55-64. [Content Brief]
[3]. Sheehan JJ, et al. Anticonvulsant effects of the BK-channel antagonist paxilline. Epilepsia. 2009 Apr;50(4):711-20. [Content Brief]
[4]. Kulawiak B, et al. Glutamate-induced cell death in HT22 mouse hippocampal cells is attenuated by paxilline, a BK channel inhibitor. Mitochondrion. 2012 Jan;12(1):169-72. [Content Brief]
[5]. Belyaeva EA, et al. Mitigating effect of paxilline against injury produced by Cd2+ in rat pheochromocytoma PC12 and ascites hepatoma AS-30D cells. Ecotoxicol Environ Saf. 2020 Jun 15;196:110519. [Content Brief]
[6]. Choi TY, et al. BK channel blocker paxilline attenuates thalidomide-caused synaptic and cognitive dysfunctions in mice. Sci Rep. 2018 Dec 5;8(1):17653. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2959 mL | 11.4795 mL | 22.9589 mL | 57.3974 mL |
| 5 mM | 0.4592 mL | 2.2959 mL | 4.5918 mL | 11.4795 mL | |
| 10 mM | 0.2296 mL | 1.1479 mL | 2.2959 mL | 5.7397 mL | |
| 15 mM | 0.1531 mL | 0.7653 mL | 1.5306 mL | 3.8265 mL | |
| 20 mM | 0.1148 mL | 0.5740 mL | 1.1479 mL | 2.8699 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9184 mL | 2.2959 mL | |
| 30 mM | 0.0765 mL | 0.3826 mL | 0.7653 mL | 1.9132 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4349 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1479 mL | |
| 60 mM | 0.0383 mL | 0.1913 mL | 0.3826 mL | 0.9566 mL | |
| 80 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL | |
| 100 mM | 0.0230 mL | 0.1148 mL | 0.2296 mL | 0.5740 mL |
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