KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC 50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.
性状
Solid
IC50 & Target[1][2]
HDAC5
体外研究(In Vitro)
KR-39038 (0-1.0 μM, 24 h) significantly inhibits angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
KR-39038 (0-30 mg/kg, Orally, once daily for 14 days) effectively attenuates both cardiac hypertrophy and dysfunction in experimental heart failure.
Pharmacokinetic Parameters of KR-39038 in Sprague-Dawley rats.
Parameters
IV (5 mg/kg)
PO (300 mg/kg)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
参考文献
[1]. Lee JH, et al. KR-39038, a Novel GRK5 Inhibitor, Attenuates Cardiac Hypertrophy and Improves Cardiac Function in Heart Failure. Biomol Ther (Seoul). 2020 Sep 1;28(5):482-489.
溶解度数据
In Vitro: DMSO : 115 mg/mL (242.11 mM; Need ultrasonic)配制储备液