2. Induced Disease Models Products Membrane Transporter/Ion Channel
  3. Nervous System Disease Models Potassium Channel
  4. Tremor Models
  5. Penitrem A

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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Penitrem A

Penitrem A Chemical Structure

CAS No. : 12627-35-9

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Penitrem A Related Antibodies

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Description

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[1][2].

IC50 & Target

BK channel[1]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
8.4 μM
Compound: 9
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
[PMID: 27462726]
HL-60 IC50
7 μM
Compound: 9
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 27462726]
In Vivo

Note:
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.

Induction of sustained tremors and at high doses convulsions and death[1][2].
Background
Biochemical effects of Penitrem A intoxication have included increase of lipids but decrease in DNA and glycogen in the liver, elevation of serum enzymes and products of anaerobic glycolysis. The serum changes were thought to be related to excess muscular activity induced by the toxin[1].
Penitrem A induced tremors might be partly explained by a presynaptic action with inhibition of inhibitory interneurons[2].
Specific Modeling Methods
Mice: ICR adult• male• weighing 38-46 g[1]
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]
Note
(1) Before the administration, the animal holding faciIitles were kept at 21°C, 50% humidity and a 12 h light-dark cycle. Mice were provided with Agway RMH 3000 pellets and water ad libitum[1][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].
Modeling Indicators
Symptoms change: Penitrem A administration demonstrated whole body tremor, weight loss and hyperexcitability. Penitrem A administration also caused the mice not to groom for 24 h[1][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].
Correlated Product(s): Diazepam; Phenobarbital; Levodopa (HY-N0304); Reserpine (HY-N0480); Pargyline (HY-A0091A)

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

634.20

Formula

C37H44ClNO6
CAS No.
Appearance

Solid

Color

White to light brown

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
Structure Classification
Initial Source

Penicillium
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5768 mL 7.8839 mL 15.7679 mL
5 mM 0.3154 mL 1.5768 mL 3.1536 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. 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 Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

SDS (479 KB)

COA (255 KB)

Handling Instructions (2659 KB)
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. 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
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Penitrem A Related Classifications

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:

Penitrem A12627-35-9Potassium ChannelKcsAInhibitorinhibitorinhibit

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