Verruculogen (Synonyms: NA 209A,TR 1) |
Catalog No.GC17001
One-Click Copy Product Info
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Maxi-K potassium channels inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 12771-72-1
Sample solution is provided at 25 µL, 10mM.
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Verruculogen is a Maxi-K potassium channels inhibitor.
Maxi-K, a potassium channel characterized by their large conductance for potassium ions through cell membranes, is activated by changes in membrane electrical potential and/or by increases in concentration of intracellular calcium ion. Maxi-K channels are critical for the regulation of several key physiological processes, such as smooth muscle tone and neuronal excitability.
In vitro: In a previous study, it was found that aflatrem, paspalitrem A, paspalitrem C, penitrem A, and paspalinine could inhibit the binding of [125I]charybdotoxin to maxi-K channels in bovine aortic smooth muscle sarcolemmal membranes. Whereas, verruculogen enhanced toxin binding. Despite their different effects on binding of [125I]charybdotoxin to maxi-K channels, all tested compounds including verruculogen were able to potently inhibit maxi-K channels in electrophysiological experiments, and other types of voltage-dependent or Ca(2+)-activated K+ channels examined were not affected [1].
In vivo: In an animal study, the mechanism of the genesis of tremor induced by verruculogen was investigated. It was found that atropine, glycine, mephenesin, and penicillamine with proven efficacy in relieving tremor of varied etiology, failed to modify verruculogen induced tremor. Oxyaminoacetic acid, which raises the CNS levels of GABA, and beta (chlorphenyl) gamma aminobutyric acid, which passes the hematoencephalic barrier, completely or partly relieved tremor and other verruculogen-induced symptoms, depending on the dose of the verruculogen administered. Picrotoxin, a GABA antagonist, increased the effect of verruculogen in the tested animals [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Knaus, H. G.,McManus, O.B.,Lee, S.H., et al. Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33(19), 5819-5828 (1994).
[2] Hotujac L, Stern P. Pharmacological examination of verruculogen induced tremor. Acta Med Iugosl. 1974;28(3):223-9.
| Cas No. | 12771-72-1 | SDF | |
| Synonyms | NA 209A,TR 1 | ||
| Chemical Name | (5R,10S,10aR)-1,10,10a,14,14aS,15bS-hexahydro-10,10a-dihydroxy-7-methoxy-2,2-dimethyl-5-(2-methyl-1-propen-1-yl)-5H,12H-3,4-dioxa-5a,11a,15a-triazacyclooct[lm]indeno[5,6-b]fluorene-11,15(2H,13H)-dione | ||
| Canonical SMILES | O=C1N2[C@](CCC2)([H])C(N3[C@@H]4C5=C(C(C=CC(OC)=C6)=C6N5[C@@H](/C=C(C)/C)OOC(C)(C)C4)[C@H](O)[C@]31O)=O | ||
| Formula | C27H33N3O7 | M.Wt | 511.6 |
| Solubility | Soluble in ethanol;Soluble in methanol;Soluble in DMSO;Soluble in dimethyl formamide | Storage | Store at -20°C; protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9547 mL | 9.7733 mL | 19.5465 mL |
| 5 mM | 390.9 μL | 1.9547 mL | 3.9093 mL |
| 10 mM | 195.5 μL | 977.3 μL | 1.9547 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)