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BU 226 hydrochloride 1186195-56-1 GlpBio

2021-08-30 来源:好走旅游网
Peptides, Inhibitors, Agonists

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Product Data Sheet

Product Name:Cat. No.:

BU 226 hydrochlorideGC15202

Chemical Properties

Cas No.ChemicalNameCanonicalSMILESFormulaSolubilityGeneral tipsShippingCondition

1186195-56-1

3-(4,5-dihydro-1H-imidazol-2-yl)isoquinoline hydrochlorideC12=CC=CC=C1C=NC(C3=NCCN3)=C2.ClC12H11N3.HCl

Soluble to 100 mM in H2O

M.WtStorage

233.7Store at RT

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bathfor a while.Stock solution can be stored below -20℃ for several months.

Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice uponrequest.

Structure

Background

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)

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@glpbio.com

Address: 10292 Central Ave. #205, Montclair, CA, USA

1www.glpbio.com

Peptides, Inhibitors, Agonists

www.glpbio.com

Product Data Sheet

is an allosteric binding site of monoamine oxidase and plays an important role in neuroprotection and painmodulation.

BU 226 hydrochloride is a selective ligand of I2 receptor. BU226 exhibited high affinity for I2 receptor with Ki value of1.4 nM and displayed 380-fold selectivity against I1 receptor. Also, BU226 showed low affinity for α2-adrenoceptor. Inrat brain or kidney membranes, BU226 showed affinity for I1, I2 receptors and α2-adrenoceptor with IC50 value of534.5 nM and Ki values of 2.7 and 6700 nM, respectively [1]. In pig brain, BU226 displaced of 2BFI with Ki value of44.7 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 adose-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 JPharmacol, 2005, 519(1-2): 68-74.

[3]. MacInnes N, Handley SL. Characterization of the discriminable stimulus produced by 2-BFI: effects of imidazolineI(2)-site ligands, MAOIs, beta-carbolines, agmatine and ibogaine. Br J Pharmacol, 2002, 135(5): 1227-1234.

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@glpbio.com

Address: 10292 Central Ave. #205, Montclair, CA, USA

2www.glpbio.com

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