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Penitrem A


CAS No. : 12627-35-9

12627-35-9
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Cat. No. : HY-N6776
M.Wt: 634.20
Formula: C37H44ClNO6
Purity: >98 %
Solubility: DMSO : ≥ 50 mg/mL
Introduction of 12627-35-9 :

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] 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)

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