Details
Stereochemistry | ACHIRAL |
Molecular Formula | C23H28N3O4S2.Na |
Molecular Weight | 497.606 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].CCCCOC(=O)[N-]S(=O)(=O)C1=C(C=C(CC(C)C)S1)C2=CC=C(CN3C=CN=C3)C=C2
InChI
InChIKey=ZUHAJKQDALIGJV-UHFFFAOYSA-M
InChI=1S/C23H29N3O4S2.Na/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);/q;+1/p-1
Molecular Formula | Na |
Molecular Weight | 22.9898 |
Charge | 1 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C23H29N3O4S2 |
Molecular Weight | 475.624 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/15537354Curator'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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15537354
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4607 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15537354 |
0.4 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Preventing | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15537354
Affinity towards AT2 receptor was evaluated in a radioligand binding assays by displacement of [125I]Ang II from AT2 receptors in pig uterus membranes. Compound M24 binds to AT2 receptor with Ki of 0.4 nM.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 13:27:27 GMT 2023
by
admin
on
Sat Dec 16 13:27:27 GMT 2023
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Record UNII |
Y151F1Q61I
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Record Status |
Validated (UNII)
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Record Version |
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Systematic Name | English |
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FDA ORPHAN DRUG |
550816
Created by
admin on Sat Dec 16 13:27:27 GMT 2023 , Edited by admin on Sat Dec 16 13:27:27 GMT 2023
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Y151F1Q61I
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126961847
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300000001701
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admin on Sat Dec 16 13:27:27 GMT 2023 , Edited by admin on Sat Dec 16 13:27:27 GMT 2023
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |
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