产品
编 号：F755916
分子式：C24H32ClFN6O
分子量：475
分子式：C24H32ClFN6O
分子量：475
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2770300-35-9
产品详情
生物活性：
KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 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.
体内研究：
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.ParametersIV (5 mg/kg) PO (300 mg/kg)
Cmax (μg/mL)NA5.2 ± 2.8
Tmax (h)NA0.7 ± 0.2
t1/2 (h)0.7 ± 0.042.3 ± 2.9
AUC0-∞ (μg*h/mL)3.4 ± 1.08.9 ± 5.0
CL (L/h/kg)1.6 ± 0.5NA
Vss (L/kg)1.2 ± 0.2NA
F (%)4.3 ± 2.4
Animal Model:C57BL/6 mice (male, 20-24 g, transverse aortic constriction)
Dosage:30 mg/kg
Administration:Orally, once a day for 2 weeks, starting from 24 h after the operation
Result:Showed a 43% reduction in the left ventricular weight, and significantly attenuated the development of cardiac hypertrophy.
Animal Model:Sprague-Dawley (S.D.) rats (male, 380-420 g, coronary artery ligation)
Dosage:10 mg/kg, 30 mg/kg
Administration:Orally, once a day for 12 weeks, starting from 24 h after surgery
Result:Showed significant preservation of cardiac function and attenuation of myocardial remodeling in a rat model of chronic heart failure following coronary artery ligation.
Animal Model:Sprague-Dawley (S.D.) rats
Dosage:5 mg/kg (IV), 300 mg/kg (Orally)
Administration:IV or Orally, single (Pharmacokinetic Analysis)
Result:The AUC∞ values after intravenous injection with 10 mg/kg and oral administration of 300 mg/kg of KR-39038 were 3.4 ± 1.0 and 8.9 ± 5.0 μg·h/mL, respectively, resulting in 4.3% bioavailability.
体外研究：
KR-39038 (0-1.0 μM, 24 h) significantly inhibits angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes.
KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 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.
体内研究：
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.ParametersIV (5 mg/kg) PO (300 mg/kg)
Cmax (μg/mL)NA5.2 ± 2.8
Tmax (h)NA0.7 ± 0.2
t1/2 (h)0.7 ± 0.042.3 ± 2.9
AUC0-∞ (μg*h/mL)3.4 ± 1.08.9 ± 5.0
CL (L/h/kg)1.6 ± 0.5NA
Vss (L/kg)1.2 ± 0.2NA
F (%)4.3 ± 2.4
Animal Model:C57BL/6 mice (male, 20-24 g, transverse aortic constriction)
Dosage:30 mg/kg
Administration:Orally, once a day for 2 weeks, starting from 24 h after the operation
Result:Showed a 43% reduction in the left ventricular weight, and significantly attenuated the development of cardiac hypertrophy.
Animal Model:Sprague-Dawley (S.D.) rats (male, 380-420 g, coronary artery ligation)
Dosage:10 mg/kg, 30 mg/kg
Administration:Orally, once a day for 12 weeks, starting from 24 h after surgery
Result:Showed significant preservation of cardiac function and attenuation of myocardial remodeling in a rat model of chronic heart failure following coronary artery ligation.
Animal Model:Sprague-Dawley (S.D.) rats
Dosage:5 mg/kg (IV), 300 mg/kg (Orally)
Administration:IV or Orally, single (Pharmacokinetic Analysis)
Result:The AUC∞ values after intravenous injection with 10 mg/kg and oral administration of 300 mg/kg of KR-39038 were 3.4 ± 1.0 and 8.9 ± 5.0 μg·h/mL, respectively, resulting in 4.3% bioavailability.
体外研究：
KR-39038 (0-1.0 μM, 24 h) significantly inhibits angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes.
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