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BU 239 hydrochloride

Catalog No.GC11580

Imidazoline receptors-selective antagonist

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BU 239 hydrochloride Chemical Structure

Cas No.: 1217041-98-9

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Target: I1 imidazoline receptor, I2 imidazoline receptor

IC50: 35 nM, 47 nM

BU 239 hydrochloride is an imidazoline receptors-selective antagonist. BU239 displayed high affinity for both I1 imidazoline and I2 imidazoline receptors in competition binding experiments with IC50 values of 35 nM and 47 nM, respectively [1]. The imidazoline receptors involved in circulatory system are classified in two groups: the I1 type and the I2 type. I1 type is sensitive to idazoxan and clonidine, an antagonist with an imidazoline structure. I2 type displays a high affinity for idazoxan, cirazoline, guanabenz and a medium-tolow affinity for clonidine. In particular, Imidazoline I1 receptors play a critical role in the central regulation of blood pressure [2].

In vitro: BU239 (1 μM) reversed α2 agonists-mediated inhibition of arginine vasopressin (AVP)-stimulated water permeability in the rat inner medullary collecting duct (IMCD) [3]. In addition, BU239 significantly reversed agmatine-induced inhibition of AVP-stimulated urea permeability (Pu) in IMCD [4]. BU239 produced positive inotropic activity with the maximum effect observed at 117.4 % [2].

In vivo: N/A

References:
1.  Flamez A, De Backer JP, Czerwiec E, Ladure P, Vauquelin G. Pharmacological characterization of I1 and I2 imidazoline receptors in human striatum. Neurochem Int. 1997;30(1):25-9.
2.  Radwanska A, Dlugokecka J, Wasilewski R, Kaliszan R. Testing conception of engagement of imidazoline receptors in imidazoline drugs effects on isolated rat heart atria. J Physiol Pharmacol. 2009;60(1):131-42.
3.  Kudo LH, Hebert CA, Rouch AJ. Inhibition of water permeability in the rat collecting duct: effect of imidazoline and alpha-2 compounds. Proc Soc Exp Biol Med. 1999;221(2):136-46.
4.  Rouch AJ, Kudo LH. Agmatine inhibits arginine vasopressin-stimulated urea transport in the rat inner medullary collecting duct. Kidney Int. 2002;62(6):2101-8.

Chemical Properties

Cas No. 1217041-98-9 SDF
Chemical Name 2-(4,5-dihydro-1H-imidazol-2-yl)quinoxaline hydrochloride
Canonical SMILES C12=CC=CC=C1N=C(C3=NCCN3)C=N2.Cl
Formula C11H10N4.HCl M.Wt 234.69
Solubility <11.73mg/ml in DMSO Storage Desiccate 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.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.2609 mL 21.3047 mL 42.6094 mL
5 mM 0.8522 mL 4.2609 mL 8.5219 mL
10 mM 0.4261 mL 2.1305 mL 4.2609 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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