BU 226 hydrochloride |
| Catalog No.GC15202 |
BU 226 염산염은 I2의 경우 Ki가 1.4nM이고 I1의 경우 IC50이 534.5nM인 선택적 이미다졸린 2(I2) 수용체 리간드입니다.
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Cas No.: 1186195-56-1
Sample solution is provided at 25 µL, 10mM.
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BU 226 hydrochloride is a selective ligand of imidazoline2 receptor [1].
Imidazoline receptor is the primary receptor for clonidine and other imidazolines. Imidazoline2 receptor (I2 receptor) is an allosteric binding site of monoamine oxidase and plays an important role in neuroprotection and pain modulation.
BU 226 hydrochloride is a selective ligand of I2 receptor. BU226 exhibited high affinity for I2 receptor with Ki value of 1.4 nM and displayed 380-fold selectivity against I1 receptor. Also, BU226 showed low affinity for α2-adrenoceptor. In rat brain or kidney membranes, BU226 showed affinity for I1, I2 receptors and α2-adrenoceptor with IC50 value of 534.5 nM and Ki values of 2.7 and 6700 nM, respectively [1]. In pig brain, BU226 displaced of 2BFI with Ki value of 44.7 nM, which suggested the presence of imidazoline I2 binding site [2].
In male Hooded Lister rats, BU226(1.6-7.0 mg/kg) potently substituted for 2-BFI with ED50 value of 3.2 mg/kg in a dose-dependent way [3].
References:
[1]. Hudson AL, Gough R, Tyacke R, et al. Novel selective compounds for the investigation of imidazoline receptors. Ann N Y Acad Sci, 1999, 881: 81-91.
[2]. Anderson NJ, Lupo PA, Nutt DJ, et al. Characterisation of imidazoline I2 binding sites in pig brain. Eur J Pharmacol, 2005, 519(1-2): 68-74.
[3]. MacInnes N, Handley SL. Characterization of the discriminable stimulus produced by 2-BFI: effects of imidazoline I(2)-site ligands, MAOIs, beta-carbolines, agmatine and ibogaine. Br J Pharmacol, 2002, 135(5): 1227-1234.
| Cas No. | 1186195-56-1 | SDF | |
| Chemical Name | 3-(4,5-dihydro-1H-imidazol-2-yl)isoquinoline hydrochloride | ||
| Canonical SMILES | C12=CC=CC=C1C=NC(C3=NCCN3)=C2.Cl | ||
| Formula | C12H11N3.HCl | M.Wt | 233.7 |
| Solubility | Soluble to 100 mM in Water | Storage | Store at RT |
| 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 | 4.279 mL | 21.395 mL | 42.7899 mL |
| 5 mM | 0.8558 mL | 4.279 mL | 8.558 mL |
| 10 mM | 0.4279 mL | 2.1395 mL | 4.279 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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