Penitrem A
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Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.
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- Pureza: 98.81%
- No. CAS: 12627-35-9
- Fòrmula: C37H44ClNO6
- Peso molecular:634.20
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Actividad biológica
BK channel[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
8.4 μM
Compound: 9
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Cytotoxicity against human A549 cells after 48 hrs by SRB assay
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
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[PMID: 27462726] |
| HL-60 | IC50 |
7 μM
Compound: 9
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Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
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[PMID: 27462726] |
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
Penitrem A can be used in animal modeling to create tremor syndrome models.
Penitrem A induced tremors might be partly explained by a presynaptic action with inhibition of inhibitory interneurons[2].
Administration: 10 mg/kg• s.c.• a single dose for 72 h or every 3 days for 18 days[1]
Rat: Naive Wistar• male• weighing 170 and 290 g[2]
Administration: 0.1 mL/100 g for i.p. or 3 μg/μL for i.c.v.• i.p. or i.c.v.• a single dose for 1, 3, 7 days[2]
(2) Penitrem A was dissolved in corn oil such that the appropriate dosage was in a volume of 2.5 mL/kg, and administered subcutaneously[1].
(3) For intraperitoneal (i.p.) injections, Penitrem A was dissolved in polyethylene glycol 300 (PEG 300) using a dose factor of 0.1 mL/100 g body weight. For intracerebroventricular (i.c.v.) administrations, Penltrem A was dissolved in 75% PEG 300, 25% saline at a concentration of 3 μg/μL[2].
Electrophysiology change: When animal was forced to move, hippocampal θ type I was largest in amplitude (254.4±19.4 instead of 182.4±36.4 mV) with some complex spikes within the first 30 min after Penltrem A injection. Intermittent high voltage spiking activities were sometime recorded after Penitrem A administration during convulsions[2].
Pathology change: Penitrem A administration had no major lesions except in the cerebellar cortex in rats. Two main types of dose-dependent lesions were observed: degeneration of Purkinje cells (PKc) and vacuolization in the molecular layer. Penitrem A induced an extensive loss of PKc and the molecular layer showed extensive vacuolization[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 12627-35-9
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Appearance Solid
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Peso molecular 634.20
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Fòrmula C37H44ClNO6
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Color White to light brown
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SMILES
O[C@]12[C@]34[C@@H]([C@H]([C@@H](C(C)=C)O[C@@]4([H])CC[C@@]1([C@]5(C(N6)=C7[C@](OC(C)([C@]8([H])[C@@]([C@]9([H])C8)(O)C%10=C7C6=CC(Cl)=C%10CC9=C)C)([H])[C@]5([H])CC2)C)C)O)O3
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Structure Classification
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Initial Source
Penicillium
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (78.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. 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)
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jortner BS, et al. Effects of prolonged tremor due to penitrem A in mice. Drug Chem Toxicol. 1986;9(2):101-16. [Content Brief]
[2]. Breton P, et al. Brain neurotoxicity of Penitrem A: electrophysiological, behavioral and histopathological study. Toxicon. 1998 Apr;36(4):645-55. [Content Brief]
[3]. Moldes-Anaya A, et al. Neurotoxicity of Penicillium crustosum secondary metabolites: tremorgenic activity of orally administered penitrem A and thomitrem A and E in mice. Toxicon. 2012 Dec 15;60(8):1428-35. [Content Brief]
[4]. Goda AA, et al. The Maxi-K (BK) Channel Antagonist Penitrem A as a Novel Breast Cancer-Targeted Therapeutic. Mar Drugs. 2018 May 11;16(5). [Content Brief]
[5]. Norris PJ, et al. Actions of tremorgenic fungal toxins on neurotransmitter release. J Neurochem. 1980 Jan;34(1):33-42. [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. 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 | 1.5768 mL | 7.8839 mL | 15.7679 mL | 39.4197 mL |
| 5 mM | 0.3154 mL | 1.5768 mL | 3.1536 mL | 7.8839 mL | |
| 10 mM | 0.1577 mL | 0.7884 mL | 1.5768 mL | 3.9420 mL | |
| 15 mM | 0.1051 mL | 0.5256 mL | 1.0512 mL | 2.6280 mL | |
| 20 mM | 0.0788 mL | 0.3942 mL | 0.7884 mL | 1.9710 mL | |
| 25 mM | 0.0631 mL | 0.3154 mL | 0.6307 mL | 1.5768 mL | |
| 30 mM | 0.0526 mL | 0.2628 mL | 0.5256 mL | 1.3140 mL | |
| 40 mM | 0.0394 mL | 0.1971 mL | 0.3942 mL | 0.9855 mL | |
| 50 mM | 0.0315 mL | 0.1577 mL | 0.3154 mL | 0.7884 mL | |
| 60 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6570 mL |
Penitrem A Related Classifications
HY-N6776 Related Classifications
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