| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
α6β2 nicotinic acetylcholine receptor (nAChR). ikB (bPiDI) is a selective antagonist for α6β2-containing nicotinic receptors. These receptors are predominantly expressed in dopaminergic neurons and play a crucial role in mediating the rewarding effects of nicotine. By binding to these receptors, bPiDI blocks the activation of α6β2 nAChRs, thereby inhibiting nicotine-induced dopamine release in the striatum. This mechanism makes it a valuable tool for studying nicotine addiction pathways.
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| ln Vitro |
In vitro, ikB (bPiDI) has been characterized using radioligand binding assays and functional electrophysiology. It selectively binds to α6β2 nAChRs with high affinity, displacing specific radioligands. In functional assays, such as calcium flux or electrophysiology in cells expressing α6β2 nAChRs, bPiDI inhibits receptor activation by acetylcholine or nicotine. It does not significantly affect other nAChR subtypes at concentrations that fully block α6β2. It inhibits nicotine-evoked dopamine release from striatal synaptosomes.
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| ln Vivo |
In vivo, ikB (bPiDI) has been studied for its effects on nicotine-evoked dopamine release. In animal models, administration of bPiDI has been shown to inhibit nicotine-induced increases in extracellular dopamine levels in the striatum, as measured by microdialysis. This confirms its in vivo activity as an α6β2 antagonist. It has potential research applications in addiction studies. Detailed in vivo efficacy and safety profiles are limited to the published literature on its mechanism.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for ikB involve radioligand binding to membrane preparations from cells expressing recombinant nAChRs. The compound is incubated with a radiolabeled ligand (e.g., [125I]α-conotoxin MII, which binds to α6-containing receptors) and membrane preparations. Non-specific binding is determined in the presence of excess unlabeled ligand. The IC50 or Ki for displacement is calculated. Selectivity is assessed by testing against other nAChR subtypes (e.g., α4β2, α7). These assays are performed in physiological buffer at room temperature.
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| Cell Assay |
In vitro cell-based assays for ikB are performed using cell lines heterologously expressing α6β2 nAChRs. Calcium flux assays are commonly used, where cells are loaded with a calcium-sensitive dye, and receptor activation by nicotine or acetylcholine is measured as an increase in fluorescence. ikB is added prior to agonist stimulation, and the inhibition of the calcium signal is measured. Electrophysiological recordings (patch-clamp) can also be used to directly measure the inhibition of nAChR-mediated currents. These assays confirm the functional antagonism of the compound.
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| Animal Protocol |
In vivo animal experiments with ikB have been conducted in rodent models. Typically, rats or mice are administered bPiDI via systemic injection (e.g., intraperitoneal). Microdialysis probes are implanted in the striatum to measure extracellular dopamine levels. Nicotine is administered, and the increase in dopamine is recorded. The effect of bPiDI pretreatment on nicotine-evoked dopamine release is assessed. These experiments demonstrate the in vivo efficacy of the compound as an α6β2 antagonist.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ikB have not been extensively reported in the available literature. As a small molecule, it is expected to have moderate lipophilicity. Its solubility and stability in biological matrices are not detailed. The compound is typically dissolved in appropriate vehicles for in vivo administration. No comprehensive ADME studies have been published. Its half-life, bioavailability, and metabolism are unknown. It is used as a research tool, and its PK properties are characterized as needed for specific experimental designs.
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| Toxicity/Toxicokinetics |
Toxicological data for ikB are not detailed in the available literature. It is a research compound not intended for human use. No LD50 values or repeated-dose toxicity studies have been reported. Standard safety pharmacology studies have not been performed. As with all research chemicals, appropriate safety precautions should be taken when handling. Its specific toxicity profile has not been established.
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| References | |
| Additional Infomation |
ikB (bPiDI) is a novel selective α6β2 nicotinic receptor antagonist. Its molecular formula is C22H34I2N2, and its molecular weight is 580.33. It is also known as bPiDI. It inhibits nicotine-evoked striatal dopamine release through an interaction with α6β2-containing nAChRs. It is a research tool for studying nicotinic receptors and addiction. It is available for research use only.
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| Molecular Formula |
C22H34N2+2.2[I-].H2O
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|---|---|
| Molecular Weight |
598.342
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| Exact Mass |
580.081
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| CAS # |
525596-64-9
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| PubChem CID |
11421854
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| Appearance |
Yellow to orange solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
26
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| Complexity |
274
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C[N+](=CC=C1)CCCCCCCCCC[N+]2=CC=CC(=C2)C.[I-].[I-]
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| InChi Key |
GMIGEVLABVAPDI-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C22H34N2.2HI/c1-21-13-11-17-23(19-21)15-9-7-5-3-4-6-8-10-16-24-18-12-14-22(2)20-24;;/h11-14,17-20H,3-10,15-16H2,1-2H3;2*1H/q+2;;/p-2
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| Chemical Name |
3-methyl-1-[10-(3-methylpyridin-1-ium-1-yl)decyl]pyridin-1-ium;diiodide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO :~100 mg/mL (~172.32 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (8.62 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5 mg/mL (8.62 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 5 mg/mL (8.62 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6713 mL | 8.3565 mL | 16.7129 mL | |
| 5 mM | 0.3343 mL | 1.6713 mL | 3.3426 mL | |
| 10 mM | 0.1671 mL | 0.8356 mL | 1.6713 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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