BU 239 hydrochlorideImidazoline receptors-selective antagonist CAS# 1217041-98-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1217041-98-9 | SDF | Download SDF |
| PubChem ID | 56846046 | Appearance | Powder |
| Formula | C11H11ClN4 | M.Wt | 234.69 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO | ||
| Chemical Name | 2-(4,5-dihydro-1H-imidazol-2-yl)quinoxaline;hydrochloride | ||
| SMILES | C1CN=C(N1)C2=NC3=CC=CC=C3N=C2.Cl | ||
| Standard InChIKey | NQMMIEICYUXMKP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C11H10N4.ClH/c1-2-4-9-8(3-1)14-7-10(15-9)11-12-5-6-13-11;/h1-4,7H,5-6H2,(H,12,13);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | High affinity ligand for the imidazoline I2 binding site. |
BU 239 hydrochloride Dilution Calculator
BU 239 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.2609 mL | 21.3047 mL | 42.6094 mL | 85.2188 mL | 106.5235 mL |
| 5 mM | 0.8522 mL | 4.2609 mL | 8.5219 mL | 17.0438 mL | 21.3047 mL |
| 10 mM | 0.4261 mL | 2.1305 mL | 4.2609 mL | 8.5219 mL | 10.6523 mL |
| 50 mM | 0.0852 mL | 0.4261 mL | 0.8522 mL | 1.7044 mL | 2.1305 mL |
| 100 mM | 0.0426 mL | 0.213 mL | 0.4261 mL | 0.8522 mL | 1.0652 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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