Chemical Structure : AZ7976
CAS No.:
2813866-27-0
AZ7976
(AZ-7976)
Catalog No.: PC-22033Not For Human Use, Lab Use Only.
AZ7976 (AZ-7976) is a potent, highly selective, allosteric relaxin family peptide receptor 1 (RXFP1) agonist with pEC50 of 9.4 in hRXFP1 cAMP assay in CHO-K1 cells, Emax=114%.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AZ7976 (AZ-7976) is a potent, highly selective, allosteric relaxin family peptide receptor 1 (RXFP1) agonist with pEC50 of 9.4 in hRXFP1 cAMP assay in CHO-K1 cells, Emax=114%.
AZ7976 binds to an allosteric site on RXFP1, does not compete with but rather enhance binding of 125I-relaxin H2.
AZ7976 is 500-fold less potent RXFP1 agonist in rat compared to human RXFP1.
AZ7976 increases heart rate achieving a Cmax at the rRXFP1cAMP EC50 elicited similar directional effects on these parameters as relaxin H2 in rodents.
Physicochemical Properties
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M.Wt
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682.65
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Formula
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C30H33F7N2O6S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(1S,4s)-4-(2-fluoro-5-(((1S,2R,3S,4R)-3-((4-fluoro-3-(pentafluoro-l6-sulfaneyl)phenyl)carbamoyl)bicyclo[2.2.1]heptan-2-yl)carbamoyl)-4-methoxyphenoxy)-1-methylcyclohexane-1-carboxylic acid
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References
1. Granberg KL, et al. J Med Chem. 2024 Mar 19. doi: 10.1021/acs.jmedchem.3c02183.
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