KR-39038 是一种口服有效的GRK5(G 蛋白偶联受体激酶 5) 抑制剂，IC50为 0.02 μM。在新生儿心肌细胞中，KR-39038 通过抑制HDAC5通路，显著抑制血管紧张素 II 诱导的细胞肥大。KR-39038 具有明显的抗心肌肥厚作用和改善心功能。KR-39038 可用于心力衰竭的研究。

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 [1].

KR-39038 (0-1.0 μM, 24 h) significantly inhibits angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes [1]. Western Blot Analysis [1] Cell Line: Primary neonatal cardiomyocytes (isolated from S.D. rats (1-2 days old) using primary myocardial cell isolation kit) Concentration: 0 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1.0 μM Incubation Time: 24 h Result: Significantly inhibited angiotensin II-induced cellular hypertrophy at a concentration of 0.1 μM and higher concentrations. Decreased angiotensin II-induced HDAC5 phosphorylation at 0.3 μM and higher concentrations.

KR-39038 (0-30 mg/kg, Orally, once daily for 14 days) effectively attenuates both cardiac hypertrophy and dysfunction in experimental heart failure [1]. Pharmacokinetic Parameters of KR-39038 in Sprague-Dawley rats [1]. Parameters IV (5 mg/kg) PO (300 mg/kg) C max (μg/mL) NA 5.2 ± 2.8 T max (h) NA 0.7 ± 0.2 t 1/2 (h) 0.7 ± 0.04 2.3 ± 2.9 AUC 0-∞ (μg*h/mL) 3.4 ± 1.0 8.9 ± 5.0 CL (L/h/kg) 1.6 ± 0.5 NA Vss (L/kg) 1.2 ± 0.2 NA F (%) 4.3 ± 2.4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years