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KR-39038
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KR-39038图片
CAS NO:2770300-35-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

KR-39038 is an orally active and potentGRK5(G protein-coupled receptor kinase 5) inhibitor, with anIC50of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression ofHDAC5pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research[1].

IC50& Target

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[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.
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[1].
Pharmacokinetic Parameters of KR-39038 in Sprague-Dawley rats[1].

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)[1]
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)[1]
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[1]
Dosage:5 mg/kg (IV), 300 mg/kg (Orally)
Administration:IV or Orally, single (Pharmacokinetic Analysis)
Result:The AUCvalues 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.
分子量

475.00

性状

Solid

Formula

C24H32ClFN6O

CAS 号

2770300-35-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

溶解性数据
In Vitro: 

DMSO : 115 mg/mL(242.11 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1053 mL10.5263 mL21.0526 mL
5 mM0.4211 mL2.1053 mL4.2105 mL
10 mM0.2105 mL1.0526 mL2.1053 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (stored under nitrogen, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。