AZ7976
AZ7976 (Compound 42) is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1) (pEC50 > 10.5). AZ7976 enhances RXFP1's cAMP signaling through an allosteric mechanism, thereby physiologically increasing heart rate. AZ7976 can be used in the field of cardiovascular disease research.
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- CAS No.: 2813866-27-0
- Formule: C30H33F7N2O6S
- Masse moléculaire:682.65
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
17 μM
Compound: 42
|
Cytotoxicity against human HepG2 cells cultured as C3a spheroids assessed as reduction in cell viability
Cytotoxicity against human HepG2 cells cultured as C3a spheroids assessed as reduction in cell viability
|
[PMID: 38502780] |
| HepG2 | IC50 |
37 μM
Compound: 42
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Cytotoxicity against human HepG2 cells cultured under galactose condition assessed as reduction in cell viability
Cytotoxicity against human HepG2 cells cultured under galactose condition assessed as reduction in cell viability
|
[PMID: 38502780] |
| HepG2 | IC50 |
68 μM
Compound: 42
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Cytotoxicity against human HepG2 cells cultured under glucose condition assessed as reduction in cell viability
Cytotoxicity against human HepG2 cells cultured under glucose condition assessed as reduction in cell viability
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[PMID: 38502780] |
| THP-1 | IC50 |
15 μM
Compound: 42
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Cytotoxicity against human THP-1 cells assessed as reduction of cell viability incubated for 48 hrs by resazurin reduction assay
Cytotoxicity against human THP-1 cells assessed as reduction of cell viability incubated for 48 hrs by resazurin reduction assay
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[PMID: 38502780] |
AZ7976 (48h) has a cytotoxicity of IC50=15 μM (THP1), 68/37 μM (HepG2 Glu/Gal), and 17 μM (HepG2 C3a spheroids). AZ7976's inhibitory effects on BSEP, hERG, NaV1.5, and KaV4.3 (Ikr) are IC50=23 μM (BSEP), >39 μM (hERG), 231 μM (NaV1.5), and >33 μM (KaV4.3 (Ikr)), respectively. In the A549 micronucleus test, it shows negative genotoxicity[1].
AZ7976 (90 min; concentration responses) does not compete with relaxin H2 for binding to RXFP1 in CHO-hRXFP1 cells, but enhances 125I-relaxin H2 binding[1].
AZ7976 inhibits ion channels and bile salt efflux transporter (BSEP) and is cytotoxic to THP1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis in AZ7976[1]
| Route | Dose (μmol/kg) | Vdss (L/kg) | Cl (mL/min/kg) | t1/2 (h) | oral dose (μmol/kg) | F (%) |
| i.v. | 0.73 | 2.3 | 38 | 2.9 | 1.46 | 11 |
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