Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H29N3O4S2 |
| Molecular Weight | 475.624 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCOC(=O)NS(=O)(=O)C1=C(C=C(CC(C)C)S1)C2=CC=C(CN3C=CN=C3)C=C2
InChI
InChIKey=XTEOJPUYZWEXFI-UHFFFAOYSA-N
InChI=1S/C23H29N3O4S2/c1-4-5-12-30-23(27)25-32(28,29)22-21(14-20(31-22)13-17(2)3)19-8-6-18(7-9-19)15-26-11-10-24-16-26/h6-11,14,16-17H,4-5,12-13,15H2,1-3H3,(H,25,27)
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25560767 |
https://www.ncbi.nlm.nih.gov/pubmed/19029468
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25560767 |
https://www.ncbi.nlm.nih.gov/pubmed/19029468
Compound M24 is a selective angiotensin II AT2 receptor agonist with a Ki value of 0.4 nM for the AT2 receptor. Compound enhances in vivo duodenal alkaline secretion in Sprague-Dawley rats, and lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats. In a mouse model of atherosclerosis, plaque size and stability were improved in ApoE‐/‐ mice treated with M24. Treatment with M24 resulted in decrease in scar size and reduction in markers of inflammation in a rat model of myocardial infaction.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Compound 21, a selective agonist of angiotensin AT2 receptors, prevents endothelial inflammation and leukocyte adhesion in vitro and in vivo. | 2016-02 |
|
| Angiotensin II type 2 receptor stimulation: a novel option of therapeutic interference with the renin-angiotensin system in myocardial infarction? | 2008-12-09 |
|
| Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist. | 2004-11-18 |
Patents
Sample Use Guides
The in vivo experiments were performed on anaesthetized nonfasted male Sprague-Dawley rats and spontaneously hypertensive rats (SHR). Compound M24 was administered intravenously at 0.003-0.3 mg/kg h. Oral PK study on rats have demonstrated absolute bioavailability of 20-30%. In the model of miocardial infarction rats were treated with M24 intraperitoneally at 0.01-0.3 mg/kg.
Route of Administration:
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9804984
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300000001702
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138409
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12498
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RC2V4W0EYC
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477775-14-7
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C190483
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
