EDG-7500 | Cardiac sarcomere modulator, Myofibril ATPase inhibitor

Chemical Structure : EDG-7500

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EDG-7500 (EDG7500)

货号: PC-28301Not For Human Use, Lab Use Only.

EDG-7500 is a diastolic-selective cardiac sarcomere modulator (d-CSM) that preferentially inhibits cardiac myofibril ATPase activity with EC25 value of 3.0 nM at diastolic calcium levels, with limited activity at systolic calcium levels (EC25>100 uM).

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生物&药学活性

EDG-7500 is a diastolic-selective cardiac sarcomere modulator (d-CSM) that preferentially inhibits cardiac myofibril ATPase activity with EC25 value of 3.0 nM at diastolic calcium levels, with limited activity at systolic calcium levels (EC25>100 uM).
EDG-7500 acts through indirect modulation of myofibril ATPase enzymatic activity that requires the regulatory light chain (RLC).
EDG-7500 preferentially inhibits DMSO normalized ATPase activity of porcine ventricle full length (VFL) myosin but do not inhibit porcine left ventricle myosin subfragment-1 (VS1).
EDG-7500 shows no inhibitory effects on DMSO normalized ATPase activity in chicken gizzard smooth muscle myofibrils.
EDG-7500 is an allosteric modulator of myosin ATPase activity dependent upon a molecular context, which requires the RLC residing within a fully intact myosin structure.
EDG-7500 shows phenotype preferentially promoting relaxation and preserving cardiac reserve without impacting systolic function in treated tissue and animals.
DG-7500 does not alter myosin SRX state, but decreases Ca2+-sensitivity of force independent of mutation in human hypertrophic cardiomyopathy (HCM) cardiac strips.
Chronic EDG-7500 normalized LV filling pressure and prevented pathological cardiac remodeling while preserving normal systolic function and cardiac reserve in R403Q swine.

物理化学性质&存储条件

分子量	389.34
分子式	C18H14F3N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-N-(1-(5-cyano-3-fluoropyridin-2-yl)ethyl)-2-(5,6-difluoro-2-oxo-1,4-dihydroquinazolin-3(2H)-yl)acetamide

参考文献

1. Li-Wen Chu E, et al. Card Fail Rev. 2025 Nov 3;11:e27.

2. Emter CA, et al. JCI Insight. 2026 Sep 22;11(18):e203086.

EDG-7500 (EDG7500)

生物&药学活性

物理化学性质&存储条件

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EDG-7500 (EDG7500)

生物&药学活性

物理化学性质&存储条件

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