KR-39038
目录号 : GC67883KR-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。
Cas No.:2770300-35-9
Sample solution is provided at 25 µL, 10mM.
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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[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) |
| Cmax (µg/mL) | NA | 5.2 ± 2.8 |
| Tmax (h) | NA | 0.7 ± 0.2 |
| t1/2 (h) | 0.7 ± 0.04 | 2.3 ± 2.9 |
| AUC0-∞ (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 |
| 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 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. |
[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.
| Cas No. | 2770300-35-9 | SDF | Download SDF |
| 分子式 | C24H32ClFN6O | 分子量 | 475 |
| 溶解度 | DMSO : 115 mg/mL (242.11 mM; Need ultrasonic) | 储存条件 | 4°C, stored under nitrogen, away from moisture |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1053 mL | 10.5263 mL | 21.0526 mL |
| 5 mM | 0.4211 mL | 2.1053 mL | 4.2105 mL |
| 10 mM | 0.2105 mL | 1.0526 mL | 2.1053 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet