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.
For research use only. We do not sell to patients.
- CAS No.: 2813866-27-0
- Formula: C30H33F7N2O6S
- Molecular Weight:682.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
|
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
|
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
|
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
|
[PMID: 38502780] |
| THP-1 | IC50 |
15 μM
Compound: 42
|
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
|
[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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