RU 28318, potassium saltPotent, selective mineralocorticoid receptor antagonist CAS# 76676-34-1 |
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Quality Control & MSDS
3D structure
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| Cas No. | 76676-34-1 | SDF | Download SDF |
| PubChem ID | 23677972 | Appearance | Powder |
| Formula | C25H37O4K | M.Wt | 440.66 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Oxprenoate potassium | ||
| Solubility | Soluble to 100 mM in water | ||
| Chemical Name | potassium;3-[(7R,8R,9S,10R,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3-oxo-7-propyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl]propanoate | ||
| SMILES | CCCC1CC2=CC(=O)CCC2(C3C1C4CCC(C4(CC3)C)(CCC(=O)[O-])O)C.[K+] | ||
| Standard InChIKey | HXJITUGMCJCKCE-UYOQDFFISA-M | ||
| Standard InChI | InChI=1S/C25H38O4.K/c1-4-5-16-14-17-15-18(26)6-10-23(17,2)19-7-11-24(3)20(22(16)19)8-12-25(24,29)13-9-21(27)28;/h15-16,19-20,22,29H,4-14H2,1-3H3,(H,27,28);/q;+1/p-1/t16-,19+,20+,22-,23+,24+,25-;/m1./s1 | ||
| 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 antagonist for the mineralocorticoid receptor (MR). Inhibits aldosterone production and secretion, and selectively decreases ex-vivo MR binding in the hippocampus of adrenalectomised rats. Also decreases blood pressure in female rats following central administration in vivo. |
RU 28318, potassium salt Dilution Calculator
RU 28318, potassium salt Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2693 mL | 11.3466 mL | 22.6932 mL | 45.3865 mL | 56.7331 mL |
| 5 mM | 0.4539 mL | 2.2693 mL | 4.5386 mL | 9.0773 mL | 11.3466 mL |
| 10 mM | 0.2269 mL | 1.1347 mL | 2.2693 mL | 4.5386 mL | 5.6733 mL |
| 50 mM | 0.0454 mL | 0.2269 mL | 0.4539 mL | 0.9077 mL | 1.1347 mL |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2269 mL | 0.4539 mL | 0.5673 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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Cardiovascular and renal effects of central administration of a mineralocorticoid receptor antagonist in conscious female rats.[Pubmed:10607876]
Eur J Pharmacol. 1999 Dec 3;385(2-3):199-202.
In a previous study we showed that in normotensive male rats brain mineralocorticoid receptor blockade induced a long lasting decrease in blood pressure associated with increased urinary excretion of water and electrolytes. Here, we report the effect of intracerebroventricular injection of a mineralocorticoid receptor antagonist (RU28318; 3,3-oxo-7 propyl-17-hydroxy-androstan-4-en-17yl-propionic acid lactone) on cardiovascular and renal function in female rats. Compared with male rats, females are less sensitive to brain mineralocorticoid receptor blockade. Administration of RU28318 (10 ng, 100 ng) caused a significant decrease in systolic blood pressure (10-12.5%) only at 8 h after injection. An increased urinary excretion of water (about 160%) and electrolytes (about 175%) during the first 8 h after the injection was observed in the 100 ng RU28318 treated group. Heart rate, food intake and water consumption were not affected at either dose. In conclusion, in conscious female rats, brain mineralocorticoid receptors participate in blood pressure and renal function control.
Evaluation of RU28318 and RU40555 as selective mineralocorticoid receptor and glucocorticoid receptor antagonists, respectively: receptor measures and functional studies.[Pubmed:9879980]
J Steroid Biochem Mol Biol. 1998 Nov;67(3):213-22.
Corticosterone regulates a wide range of physiological parameters. Two receptors for corticosterone have been identified, the mineralocorticoid (type I) receptor (MR) and the glucocorticoid (type II) receptor (GR). To determine the relative role of these two receptors in mediating the effects of endogenous corticosterone, many studies have relied on the use of putative selective corticosteroid receptor antagonists. This study further examined the in vivo receptor selectivity of two compounds, RU28318 and RU40555 that are believed to be selective antagonists for MR and GR, respectively. Acute treatment of adrenalectomized rats with RU28318 (10-50 mg/kg) selectively decreased ex-vivo available MR binding in the hippocampus, whereas acute treatment with RU40555 (10-30 mg/kg) selectively decreased available GR binding in the hippocampus and pituitary. These receptor binding measures suggest that RU28318 in vivo selectively occupied MR, and that RU40555 in vivo selectively occupied GR. In functional studies, RU28318 (50 mg/kg) blocked the normalizing effect of aldosterone (120 microg/kg) on saline intake of adrenalectomized rats. RU40555 (30 mg/kg) blocked the suppressive effect of dexamethasone (50 microg/kg) on acute stress-induced corticosterone secretion. These studies further support the in vivo corticosteroid receptor selectivity of these two compounds and confirms their effective corticosteroid antagonistic properties.
The effect of the antimineralocorticoid RU 28318 on aldosterone biosynthesis in vitro.[Pubmed:6323881]
J Steroid Biochem. 1984 Apr;20(4A):853-6.
The effect of RU 28318, a specific and highly potent aldosterone antagonist on mineralocorticoid biosynthesis has been studied using a new in vitro model which combined three original features: (1) a very specific radioimmunoassay for aldosterone (2) a simplified perifusion system and (3) frog interrenal tissue which spontaneously produces high amounts of aldosterone. A dose-related inhibition of aldosterone production was observed for doses ranging from 10(-5) to 10(-3) M of RU 28318. The intermediate dose of 10(-4) M caused 71% inhibition of aldosterone production. Long term infusion of RU 28318 for 8 h led to a significant, stable and reversible inhibition of aldosterone production. In addition, we provide evidence that RU 28318 is capable of blocking the stimulation of aldosterone secretion induced by synthetic ACTH or by angiotensin II analogue. The present results demonstrate that RU 28318 is responsible for a significant and reversible inhibition of spontaneous, ACTH-induced and angiotensin II-induced aldosterone biosynthesis in vitro.
