KR-39038
目录号: PL03996 纯度: ≥98%
CAS No. :2770300-35-9
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中文名称
KR-39038
英文名称
KR-39038
英文别名
4(3H)-Quinazolinone, 7-[[3-[[4-[(3-aminopropyl)amino]butyl]amino]propyl]amino]-2-(2-chlorophenyl)-6-fluoro-;KR-39038
Cas No.
2770300-35-9
分子式
C24H32ClFN6O
分子量
475.00
包装储存
4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
产品详情
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 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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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