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Efaroxan hydrochloride

CAS# 89197-00-2

Efaroxan hydrochloride

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Chemical structure

Efaroxan hydrochloride

3D structure

Chemical Properties of Efaroxan hydrochloride

Cas No. 89197-00-2 SDF Download SDF
PubChem ID 11957548 Appearance Powder
Formula C13H17ClN2O M.Wt 252.74
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water
Chemical Name 2-(2-ethyl-3H-1-benzofuran-2-yl)-4,5-dihydro-1H-imidazole;hydrochloride
SMILES CCC1(CC2=CC=CC=C2O1)C3=NCCN3.Cl
Standard InChIKey DWOIUCRHVWIHAH-UHFFFAOYSA-N
Standard InChI InChI=1S/C13H16N2O.ClH/c1-2-13(12-14-7-8-15-12)9-10-5-3-4-6-11(10)16-13;/h3-6H,2,7-9H2,1H3,(H,14,15);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.
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.
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.

Biological Activity of Efaroxan hydrochloride

DescriptionPotent, highly selective α2 adrenoceptor antagonist and imidazoline I1 receptor ligand (pKi values are 7.87, 7.42, 5.74, 7.28 and < 5 for α 2A, α2B, α2C, I1, and I2 receptors respectively). Promotes insulin secretion, at a site distinct from I1 or I2 (the putative I3 receptor) in vitro and in vivo.

Efaroxan hydrochloride Dilution Calculator

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Preparing Stock Solutions of Efaroxan hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.9566 mL 19.7832 mL 39.5664 mL 79.1327 mL 98.9159 mL
5 mM 0.7913 mL 3.9566 mL 7.9133 mL 15.8265 mL 19.7832 mL
10 mM 0.3957 mL 1.9783 mL 3.9566 mL 7.9133 mL 9.8916 mL
50 mM 0.0791 mL 0.3957 mL 0.7913 mL 1.5827 mL 1.9783 mL
100 mM 0.0396 mL 0.1978 mL 0.3957 mL 0.7913 mL 0.9892 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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References on Efaroxan hydrochloride

Effects of the imidazoline ligands efaroxan and KU14R on blood glucose homeostasis in the mouse.[Pubmed:12409010]

Eur J Pharmacol. 2002 Nov 1;454(1):95-102.

The putative imidazoline I(3) receptor antagonist 2-(2-ethyl-2,3-dihydrobenzo[b]furan-2-yl)-1H-imidazole (KU14R) has been shown to block the effects of the atypical I(3) agonist efaroxan at the level of the ATP-sensitive K(+) (K(ATP)) channel in isolated pancreatic islet beta cells, but its effects in vivo are not known. We have therefore investigated the effects of KU14R on blood glucose and insulin level in vivo. When KU14R was administered before or after a hypoglycaemic dose of efaroxan, the fall in blood glucose was at least additive. When the antihyperglycaemic imidazoline ligand S22068 was administered after a dose of KU14R, it did not alter the hypoglycaemic response. In the mouse isolated vas deferens preparation, neither rauwolscine (at concentrations which competitively antagonised the inhibitory response to 5-bromo-6-(2-imidazolin-2-ylamino)-quinoxaline (UK14304)) nor KU14R affected inhibition produced by S22068. At 10(-4) M, KU14R had weak alpha(2)-adrenoceptor antagonist activity. We conclude that KU14R does not act as an antagonist of either efaroxan or S22068 at an imidazoline site in vivo.

'Seeing through a glass darkly': casting light on imidazoline 'I' sites.[Pubmed:9786027]

Trends Pharmacol Sci. 1998 Sep;19(9):381-90.

Although imidazoline sites have been the subject of research for several years, there is still controversy about their structure, diversity and physiology. The I1 site is thought to exist principally as a binding site and is widely purported to play a role in controlling systemic blood pressure, although this is still unclear. The majority of I2 sites are widely accepted as being allosteric sites on monoamine oxidase; however, even with selective ligands, their exact function remains to be determined. A putative I3 site modulates insulin secretion and could represent the first functional site to be pharmacologically defined with selective agonists and antagonists. The structure and relevance of the proposed endogenous ligand 'clonidine-displacing substance' remains elusive. A potential candidate for this substance is agmatine; however, although it is capable of displacing bound clonidine from imidazoline sites, it lacks the functionality ascribed to the clonidine-displacing substance. In this review, Richard M. Eglen and colleagues assess our knowledge of imidazoline sites in the light of recent data.

Imidazolines stimulate release of insulin from RIN-5AH cells independently from imidazoline I1 and I2 receptors.[Pubmed:7813577]

Eur J Pharmacol. 1994 Sep 1;262(1-2):41-8.

The effect on insulin release of efaroxan, an alpha 2-adrenoceptor antagonist and a highly potent drug at imidazoline I1 receptors, and the effects of seven other imidazoline compounds selective for the imidazoline I1 or I2 receptors, were studied in the rat insulinoma cell line RIN-5AH. The cells released insulin in response to glucose (0.3-10 mM), and efaroxan (100 microM) potentiated glucose-induced insulin release. (-)-Adrenaline completely displaced the binding of [125I]p-iodoclonidine to membranes of RIN-5AH cells, indicating that these cells do not express imidazoline I1 receptors. Cirazoline and idazoxan (100 microM), both highly potent drugs at imidazoline I2 receptors, and the guanidines guanoxan and amiloride (200 microM), also promoted insulin release from RIN-5AH cells. Irreversible blockade of imidazoline I2 receptors with 10 microM clorgyline did not prevent the stimulatory effects of cirazoline or idazoxan; however, these compounds completely reversed the inhibition by diazoxide (250 microM), an opener of ATP-dependent K+ channels (K+ATP channels), of glucose-induced insulin release. These data indicate that the imidazoline/guanidine compounds promote insulin release from RIN-5AH cells, by interacting with a novel binding site related to K+ATP channels that does not represent any of the known imidazoline I1 or I2 receptors.

Alpha-adrenoreceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on alpha-adrenoreceptor activity.[Pubmed:6143826]

J Med Chem. 1984 May;27(5):570-6.

Modification of the 1,4-benzodioxan ring present in RX 781094 has not previously been considered. This paper describes a number of analogues of this ring system, including compounds in which one of the oxygen atoms has been replaced by a methylene group and also those in which the ring size has been changed to give, for example, furan and thiophene derivatives. The dihydrobenzofuranylimidazoline compound 7 is the only analogue possessing presynaptic antagonist potency potency and selectivity comparable to that of 1. In view of this result, a number of derivatives was prepared to determine the structure-activity relationships within this series. Many derivatives, as well as the parent compound 7, were found to possess presynaptic alpha 2-adrenoreceptor antagonist and postsynaptic alpha 1-adrenoreceptor partial agonist properties. Two of the selective presynaptic antagonists, 13 and 14 possess greater potency and selectivity than that possessed by 1. The 5-chloro derivative 25 is twice as potent as after oral administration but only about half as potent when given intravenously.

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