2. GPCR/G Protein
  3. RXFP Receptor
  4. 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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AZ7976

AZ7976 화학구조

CAS No. : 2813866-27-0

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제품 설명

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[1].

Cellular Effect
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]
In Vitro

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.

AZ7976 Related Antibodies
In Vivo

AZ7976 (i.v.; initial 1.5 mg/kg; i.v.drip; continuous 9.0 mg/kg) causes a significant increase in heart rate and a rise in mean arterial blood pressure in the rats.[1].

Pharmacokinetic Analysis in AZ7976[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Animal Model: Sprague-Dawley rats[1]
Dosage: initial 1.5 mg/kg, continuous 9.0 mg/kg
Administration: i.v.; i.v.drip
Result: Caused a significant increase in heart rate and a rise in mean arterial blood pressure in the rats, the same response in Sprague-Dawley rats as after RXFP1 receptor activation
분자량

682.65

화학식

C30H33F7N2O6S
CAS No.
SMILES

COC1=CC(F)=C(C=C1C(N[C@H]2[C@H]([C@@H]3CC[C@H]2C3)C(NC4=CC=C(C(S(F)(F)(F)(F)F)=C4)F)=O)=O)O[C@H]5CC[C@](C)(CC5)C(O)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
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AZ7976 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ79762813866-27-0AZ 7976AZ-7976RXFP ReceptorRelaxin family peptideRXFP1 AgonistCardiovascular EffectsAllosteric ModulationInhibitorinhibitorinhibit

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상품명:
AZ7976
Cat. No.:
HY-162401
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