Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C25H38O4 |
Molecular Weight | 402.5668 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 7 / 7 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@@](O)(CCC(O)=O)[C@@]1(C)CC[C@@]3([H])[C@@]2([H])[C@H](CCC)CC4=CC(=O)CC[C@]34C
InChI
InChIKey=DNHCHRGCTVRAFT-JEHIOXJOSA-N
InChI=1S/C25H38O4/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)/t16-,19+,20+,22-,23+,24+,25-/m1/s1
RU 28318 also known as OXPRENOATE is a mineralocorticoid receptor (MR) antagonist, inhibiting aldosterone production and secretion. RU 28318 has been studied in normal and diabetic rats. It was revealed, that in combination with angiotensin converting enzyme inhibitors, RU 28318 was the most effective at improving -dP/dt (a measure of diastolic function) and attenuated cardiac dysfunction in diabetes.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1994 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9879980 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Evaluation of RU28318 and RU40555 as selective mineralocorticoid receptor and glucocorticoid receptor antagonists, respectively: receptor measures and functional studies. | 1998 Nov |
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Direct targeting of hippocampal neurons for apoptosis by glucocorticoids is reversible by mineralocorticoid receptor activation. | 2005 Aug |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18227408
Heart failure (HF) rats: treated for 4 weeks with intracerebroventricular RU28318 (1 μg/hr) had less hypothalamic ACE and AT1-R mRNA and protein, less NAD(P)H-induced superoxide in PVN, fewer excited PVN neurons, and lower plasma NE. RU28318 had no effect on plasma ALDO, or on ACE or AT1-R mRNA expression in brain cortex
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24066305
Hearts removed from animals were perfused for 30 min and then subjected to 30 min of global ischemia (I) followed by a period of 30 min of reperfusion (R). Drugs were administered for 30 min either during perfusion before ischemia or during reperfusion after ischemia. Drug regimens tested were RU28318 (RU; 10-5 M), Captopril (Capt; 3.6 × 10-4 M), Losartan (Los; 3 × 10-4 M), RU + Capt, RU + Los, Capt + Los, and RU + Capt + Los (Triple). In ischemia/reperfusion- (I/R-) injury, was shown that combination approaches were better where Capt + Los + RU (Triple) therapy used in normal and diabetes. However, combination therapies with ACEI and ARBs are rarely employed in the clinic possibly due to fear over accumulating adverse effects in patients with heart disorders.
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NCI_THESAURUS |
C448
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786592-95-8
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3034004
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C87707
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Oxprenoic acid
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DTXSID90229228
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2JGY63UVRO
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)