3-Bromocytisine
Based on 1 Customer Validation
3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC50s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC50s are 8 and 50 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 207390-14-5
- Formula: C11H13BrN2O
- Molecular Weight:269.14
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 0.28 nM (hα4β4), 0.30 nM (hα4β2), 31.6 nM (hα7)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-32 | IC50 |
15.6 nM
Compound: 3-bromocytisine
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Displacement of [3H]epibatidine from alpha3 nAChR in human IMR32 cells
Displacement of [3H]epibatidine from alpha3 nAChR in human IMR32 cells
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[PMID: 19576766] |
| IMR-32 | IC50 |
15.6 nM
Compound: 3-Bromocytisine
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Displacement of [3H]epibatidine from alpha3beta4 nAChR expressed in IMR32 cells
Displacement of [3H]epibatidine from alpha3beta4 nAChR expressed in IMR32 cells
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[PMID: 20043678] |
Chemical Information
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CAS No. 207390-14-5
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Appearance Solid
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Molecular Weight 269.14
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Formula C11H13BrN2O
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Color White to off-white
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SMILES
O=C1N2C([C@]3([H])C[C@](CNC3)([H])C2)=CC=C1Br
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Synonyms
3-Br-cytisine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (371.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Houlihan LM, et al. Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors. J Neurochem. 2001 Sep;78(5):1029-43. [Content Brief]
[2]. Moroni M, et al. alpha4beta2 nicotinic receptors with high and low acetylcholine sensitivity: pharmacology, stoichiometry, and sensitivity to long-term exposure to nicotine. Mol Pharmacol. 2006 Aug;70(2):755-68. [Content Brief]
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 | 3.7155 mL | 18.5777 mL | 37.1554 mL | 92.8885 mL |
| 5 mM | 0.7431 mL | 3.7155 mL | 7.4311 mL | 18.5777 mL | |
| 10 mM | 0.3716 mL | 1.8578 mL | 3.7155 mL | 9.2888 mL | |
| 15 mM | 0.2477 mL | 1.2385 mL | 2.4770 mL | 6.1926 mL | |
| 20 mM | 0.1858 mL | 0.9289 mL | 1.8578 mL | 4.6444 mL | |
| 25 mM | 0.1486 mL | 0.7431 mL | 1.4862 mL | 3.7155 mL | |
| 30 mM | 0.1239 mL | 0.6193 mL | 1.2385 mL | 3.0963 mL | |
| 40 mM | 0.0929 mL | 0.4644 mL | 0.9289 mL | 2.3222 mL | |
| 50 mM | 0.0743 mL | 0.3716 mL | 0.7431 mL | 1.8578 mL | |
| 60 mM | 0.0619 mL | 0.3096 mL | 0.6193 mL | 1.5481 mL | |
| 80 mM | 0.0464 mL | 0.2322 mL | 0.4644 mL | 1.1611 mL | |
| 100 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9289 mL |
3-Bromocytisine Related Classifications
HY-107684 Related Classifications
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