Pozanicline dihydrochloride
Based on 1 Customer Validation
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
For research use only. We do not sell to patients.
- Purity: 99.06%
- CAS No.: 161416-61-1
- Formula: C11H18Cl2N2O
- Molecular Weight:265.18
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Pozanicline (ABT-089) is a partial agonist at α4β2 nAChR. Moreover, one α6β2 nAChR subtype is particularly sensitive to Pozanicline with an EC50 of 0.11 μM[2].
Pozanicline (ABT-089) shows high selectivity for α6β2 and α4α5β2 nAChR subtypes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male C57BL6/J mice at 8-12 weeks of age[3].
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Dosage:0.3 mg/kg and 0.6 mg/kg
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Administration:Treated 5 min before training and testing for contextual fear conditioning
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Result:A dose of 0.3 mg/kg and 0.6 mg/kg ameliorated nicotine withdrawal-induced cognitive deficits in contextual fear conditioning.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 161416-61-1
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Appearance Solid
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Molecular Weight 265.18
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Formula C11H18Cl2N2O
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Color White to off-white
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SMILES
[H]Cl.[H]Cl.CC(N=CC=C1)=C1OC[C@@H]2CCCN2
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Synonyms
ABT-089 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 100 mg/mL (377.10 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (377.10 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lin NH, et al. Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties. J Med Chem. 1997 Jan 31;40(3):385-90 [Content Brief]
[2]. Marks MJ, et al. Selectivity of ABT-089 for α4β2 and α6β2 nicotinic acetylcholine receptors in brain. Biochem Pharmacol. 2009 Oct 1;78(7):795-802. [Content Brief]
[3]. Yildirim E, et al. ABT-089, but not ABT-107, ameliorates nicotine withdrawal-induced cognitive deficits in C57BL6/J mice. Behav Pharmacol. 2015 Apr;26(3):241-8. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 3.7710 mL | 18.8551 mL | 37.7102 mL | 94.2756 mL |
| 5 mM | 0.7542 mL | 3.7710 mL | 7.5420 mL | 18.8551 mL | |
| 10 mM | 0.3771 mL | 1.8855 mL | 3.7710 mL | 9.4276 mL | |
| 15 mM | 0.2514 mL | 1.2570 mL | 2.5140 mL | 6.2850 mL | |
| 20 mM | 0.1886 mL | 0.9428 mL | 1.8855 mL | 4.7138 mL | |
| 25 mM | 0.1508 mL | 0.7542 mL | 1.5084 mL | 3.7710 mL | |
| 30 mM | 0.1257 mL | 0.6285 mL | 1.2570 mL | 3.1425 mL | |
| 40 mM | 0.0943 mL | 0.4714 mL | 0.9428 mL | 2.3569 mL | |
| 50 mM | 0.0754 mL | 0.3771 mL | 0.7542 mL | 1.8855 mL | |
| 60 mM | 0.0629 mL | 0.3143 mL | 0.6285 mL | 1.5713 mL | |
| 80 mM | 0.0471 mL | 0.2357 mL | 0.4714 mL | 1.1784 mL | |
| 100 mM | 0.0377 mL | 0.1886 mL | 0.3771 mL | 0.9428 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.