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| Targets |
Penitrem A targets the large-conductance calcium-activated potassium channel KCa1.1, also known as the BK (big potassium) channel. BK channels are voltage- and calcium-activated potassium channels that play important roles in the regulation of neuronal excitability, smooth muscle tone, and neurotransmitter release. Penitrem A is a selective, irreversible blocker of the BK channel. It inhibits the binding of charybdotoxin, a well-known BK channel blocker, with an IC50 value of 1.7 microM. Penitrem A can stimulate cerebral cortical synaptosomes to increase the spontaneous release of endogenous glutamate, GABA, and aspartate. It can induce tremor syndrome in animals.
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| ln Vitro |
Penitrem A demonstrates potent in vitro activity as a BK channel blocker. The compound inhibits the binding of charybdotoxin to BK channels with an IC50 value of 1.7 microM. It is a selective, irreversible blocker of the smooth muscle high-conductance Ca2+-activated K+ channel. Penitrem A has anti-proliferative and anti-invasive effects on a variety of malignant tumors. The compound's activity is concentration-dependent. It is used as a tool to evaluate the role of BK channel-mediated potassium flux in various cell processes and responses. Penitrem A can stimulate cerebral cortical synaptosomes to increase the spontaneous release of neurotransmitters.
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| ln Vivo |
Tremor syndrome models can be created using Penitem A in animal modeling.
In vivo, Penitrem A is a tremorgenic mycotoxin that can induce tremor syndrome in animals. It affects mammals primarily through inhibition of neurotransmitter release. The compound's neurotoxic properties are characterized by tremors and neurological effects. Penitrem A is used to evaluate the role of BK channels in vascular function, which is effective in cellular, tissue, and physiological studies. As a mycotoxin, Penitrem A is also of toxicological interest for its effects on the nervous system. Its ability to stimulate neurotransmitter release contributes to its neurotoxic effects. |
| Enzyme Assay |
In vitro receptor binding assays for Penitrem A involve measuring binding affinity to the BK channel (KCa1.1). Membranes from cells expressing BK channels are incubated with a radiolabeled BK channel ligand (e.g., [¹2⁵I]-charybdotoxin) and varying concentrations of the test compound. Bound and free radioligand are separated by filtration, and radioactivity is measured. Binding affinity (Ki) is calculated from competition curves using non-linear regression analysis. The compound inhibits charybdotoxin binding with an IC50 of 1.7 microM. Functional assays can measure inhibition of BK channel-mediated potassium flux using electrophysiological techniques such as patch-clamp recording. Each concentration is typically tested in duplicate or triplicate.
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| Cell Assay |
In vitro cellular assays for Penitrem A are performed using cells expressing BK channels or primary neurons. Electrophysiological recordings using patch-clamp techniques are used to measure BK channel currents and the effects of Penitrem A on channel activity. Alternatively, ion flux assays using fluorescent potassium indicators or radioactive tracers can be used. In neuronal cultures, the compound's effects on neurotransmitter release can be assessed by measuring glutamate, GABA, or aspartate levels in the culture medium. In cancer cell lines, anti-proliferative and anti-invasive effects are assessed using cell viability, proliferation, and migration assays. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. EC50 or IC50 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for Penitrem A are conducted to study its neurotoxic and tremorgenic effects. Rodents are administered Penitrem A via intraperitoneal injection or oral administration. Tremor syndrome is assessed by observing and scoring tremor intensity and duration. Neurological effects are monitored. In toxicology studies, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. The compound's effects on neurotransmitter release and BK channel function can be assessed in brain tissue samples. Penitrem A is used as a tool to study the role of BK channels in vivo. Comprehensive toxicological characterization has been conducted as part of mycotoxin research.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Penitrem A have been characterized in toxicology studies. The compound has a molecular formula of C37H44ClNO6 and a molecular weight of 634.20 g/mol. It is a lipophilic compound that can cross the blood-brain barrier, consistent with its neurotoxic effects. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in animal models. The compound's ability to reach the central nervous system is relevant for its tremorgenic effects. Its pharmacokinetic profile supports its use as a research tool for studying BK channel function and neurotoxicity.
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| Toxicity/Toxicokinetics |
Penitrem A is a potent mycotoxin with significant neurotoxicity. As a tremorgenic toxin, it induces tremor syndrome in animals. The compound is a selective, irreversible blocker of BK (KCa1.1) channels. Standard toxicology studies have characterized the compound's effects on the nervous system. The compound's neurotoxic properties require careful handling and safety precautions. Penitrem A is not approved for human use and is strictly intended for research purposes as a pharmacological tool.
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| References | |
| Additional Infomation |
Penitrem A is an oxygen-containing organic compound and an organic heterocyclic tricyclic compound. It has been reported to exist in Mucor irregularis, Penicillium canescens, and other organisms with relevant data.
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium species. It is a selective, irreversible blocker of the BK (KCa1.1) channel, inhibiting charybdotoxin binding with an IC50 of 1.7 microM. Penitrem A has anti-proliferative and anti-invasive effects on various malignant tumors. It can stimulate neurotransmitter release and induce tremor syndrome in animals. The compound has a molecular formula of C37H44ClNO6 and a molecular weight of 634.20 g/mol. Penitrem A has not entered clinical trials and is available for research purposes only. It is a valuable tool for studying BK channel function and neurotoxicity. |
| Molecular Formula |
C37H44NO6CL
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| Molecular Weight |
634.20136
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| Exact Mass |
633.285
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| CAS # |
12627-35-9
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| PubChem CID |
6610243
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| Appearance |
White to light brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.698
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| LogP |
6.46
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
45
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| Complexity |
1420
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| Defined Atom Stereocenter Count |
13
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| SMILES |
CC(=C)[C@@H]1[C@@H]([C@@H]2[C@@]3(O2)[C@@H](O1)CC[C@]4([C@]3(CC[C@@H]5[C@@]4(C6=C7[C@H]5OC([C@H]8C[C@H]9[C@@]8(C1=C7C(=CC(=C1CC9=C)Cl)N6)O)(C)C)C)O)C)O
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| InChi Key |
JDUWHZOLEDOQSR-JKPSMKLGSA-N
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| InChi Code |
InChI=1S/C37H44ClNO6/c1-15(2)28-27(40)31-37(45-31)23(43-28)9-10-33(6)34(7)18(8-11-35(33,37)41)29-25-24-21(39-30(25)34)14-20(38)17-12-16(3)19-13-22(32(4,5)44-29)36(19,42)26(17)24/h14,18-19,22-23,27-29,31,39-42H,1,3,8-13H2,2,4-7H3/t18-,19+,22+,23-,27-,28+,29-,31+,33+,34+,35-,36+,37-/m0/s1
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| Chemical Name |
(1S,2R,5S,6S,8R,9S,10R,12S,15R,16S,25R,27S,28R)-21-chloro-15,16,33,33-tetramethyl-24-methylidene-10-prop-1-en-2-yl-7,11,32-trioxa-18-azadecacyclo[25.4.2.02,16.05,15.06,8.06,12.017,31.019,30.022,29.025,28]tritriaconta-17(31),19,21,29-tetraene-5,9,28-triol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1577 mL | 0.7884 mL | 1.5768 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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