SKF 86466 hydrochlorideCAS# 86129-54-6 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 86129-54-6 | SDF | Download SDF |
| PubChem ID | 10220250 | Appearance | Powder |
| Formula | C11H15Cl2N | M.Wt | 232.15 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water and to 100 mM in DMSO | ||
| Chemical Name | 6-chloro-3-methyl-1,2,4,5-tetrahydro-3-benzazepine;hydrochloride | ||
| SMILES | CN1CCC2=C(CC1)C(=CC=C2)Cl.Cl | ||
| Standard InChIKey | JKQKVNMNAIFCFS-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C11H14ClN.ClH/c1-13-7-5-9-3-2-4-11(12)10(9)6-8-13;/h2-4H,5-8H2,1H3;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 | Potent and selective α2 antagonist at pre- and post-junctional α2-adrenoceptors (Ki values are 13 and 17 nM respectively). Exhibits antihypertensive activity in a rat model. |
SKF 86466 hydrochloride Dilution Calculator
SKF 86466 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.3076 mL | 21.5378 mL | 43.0756 mL | 86.1512 mL | 107.689 mL |
| 5 mM | 0.8615 mL | 4.3076 mL | 8.6151 mL | 17.2302 mL | 21.5378 mL |
| 10 mM | 0.4308 mL | 2.1538 mL | 4.3076 mL | 8.6151 mL | 10.7689 mL |
| 50 mM | 0.0862 mL | 0.4308 mL | 0.8615 mL | 1.723 mL | 2.1538 mL |
| 100 mM | 0.0431 mL | 0.2154 mL | 0.4308 mL | 0.8615 mL | 1.0769 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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An evaluation of the alpha-adrenoceptor antagonism produced by SK&F 86466 in healthy normotensive males.[Pubmed:1981137]
Br J Clin Pharmacol. 1990 Dec;30(6):884-8.
SK&F 86466 is a novel, potent alpha-adrenoceptor antagonist which, in animal experiments, is reported to show a high selectivity for alpha 2-adrenoceptors at both pre- and post-junctional sites. The effects of two intravenous doses of 80 and 200 micrograms kg-1 of SK&F 86466 were assessed in a placebo-controlled, double-blind, randomised study in eight young, healthy, normotensive males. Two indices of alpha-adrenoceptor activity were investigated: i) Pressor responsiveness to the relatively selective alpha 1-adrenoceptor agonist phenylephrine and to the preferential alpha 2-adrenoceptor agonist alpha-methylnoradrenaline. ii) Circulating levels of noradrenaline. SK&F 86466 at a dose of 200 micrograms kg-1 produced rightward shifts of the pressor dose-response curves to both agonists: a 1.4 fold shift for phenylephrine (P = 0.023) and a 1.6 fold shift for alpha-methylnoradrenaline (P = 0.051). Erect plasma noradrenaline sampled at 105 min into the infusion was significantly increased from 2.9 to 5.0 nmol l-1 by SK&F 86466 200 micrograms kg-1 (P = 0.002). The change in the phenylephrine responses indicates post-junctional alpha 1-adrenoceptor blockade and the rise in noradrenaline is consistent with pre-junctional alpha 2-adrenoceptor antagonist activity. Overall the results of this study suggest that SK&F 86466, at a dose of 200 micrograms kg-1, causes both alpha 1- and alpha 2-adrenoceptor antagonism in human subjects.
Characterization of the antihypertensive activity of SK&F 86466, a selective alpha-2 antagonist, in the rat.[Pubmed:2867209]
J Pharmacol Exp Ther. 1986 Jan;236(1):1-7.
The effects of SK&F 86466 (6-chloro-N-methyl-2,3,4,5-tetrahydro-1-H-3-benzazepine), a potent and selective alpha-2 adrenoceptor antagonist, on blood pressure and heart rate were examined in normotensive and hypertensive rats. SK&F 86466 was approximately 10-fold more potent in lowering blood pressure in deoxycorticosterone acetate (DOCA)-salt hypertensive than in normotensive rats, when administered by i.v. infusion. A dose-related antihypertensive effect was observed in conscious DOCA-salt rats after p.o. doses of SK&F 86466 (2-15 mg/kg), with a duration of over 6 hr after the highest dose. Oral administration of SK&F 86466 was associated with tachycardia, which reached maximal levels within 15 min after dosing, followed by an interval of bradycardia. The duration of antihypertensive activity observed with SK&F 86466 was at least 6 hr, compared to less than 90 min with phentolamine, at doses which produced equal peak reductions in blood pressure in conscious DOCA-salt rats. In contrast, heart rate was still significantly elevated by phentolamine 90 min postdosing, whereas the transient tachycardia induced by SK&F 86466 had dissipated within 30 min. SK&F 86466 was also an effective antihypertensive agent in the spontaneously hypertensive rat, although lower antihypertensive efficacy was observed than in the DOCA-salt model. SK&F 86466 was even less effective in the two-kidney one-clip Goldblatt model in which hypertension is maintained by the renin-angiotensin system rather than by the sympathetic nervous system.(ABSTRACT TRUNCATED AT 250 WORDS)
