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AR 244555
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H23ClF2N2O
- MW: 416.89
Description
AR 244555 is an inverse agonist of Mas receptor G-protein signaling with reported IC50 values of 186 nM and 348 nM in human and rat inositol phosphate Gq-coupling assays. It inhibits Mas-associated inositol 1,4,5-trisphosphate accumulation and cardiac cell enlargement phenotypes.
The Mas receptor is part of the renin-angiotensin system and participates in cardiovascular signaling, coronary flow and ischemia-reperfusion responses. AR 244555 is relevant for probing basal and ligand-dependent Mas receptor activity.
Key Features
- Mas receptor inverse agonist
- Inhibits Gq/IP signaling in human and rat assays
- Modulates Mas-overexpression cardiac phenotypes
- Reported protective effects in ischemia-reperfusion models
Applications
- Mas receptor pharmacology
- Renin-angiotensin system research
- Cardiac ischemia-reperfusion studies
- GPCR inverse agonism assays
More Information
| Parent CAS No. | 858350-62-6 |
|---|---|
| Chemical Name | (1'-(but-3-enyl)-5-chlorospiro[indoline-3,4'-piperidine]-1-yl)(2,6-difluorophenyl)methanone |
| SMILES | C1(Cl)C=C2C3(CCN(CCC=C)CC3)CN(C(C3C(F)=CC=CC=3F)=O)C2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C23H23ClF2N2O/c1-2-3-11-27-12-9-23(10-13-27)15-28(20-8-7-16(24)14-17(20)23)22(29)21-18(25)5-4-6-19(21)26/h2,4-8,14H,1,3,9-13,15H2 |
| InChiKey | QKPSTNGNDWHYCH-UHFFFAOYSA-N |
| CID | 59004159 |
| Short Description | Mas inverse agonist |
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