计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,充氩,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
In Vitro
KR-39038 (0-1.0 μM, 24 h) significantly inhibits angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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.
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) 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 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
Form:Solid
IC50& Target:HDAC5
规格
规格或纯度
≥98%
英文名称
KR-39038
生化机理
KR-39038 是一种具有口服活性的强效 GRK5（G 蛋白偶联受体激酶 5）抑制剂，其 IC 50 为 0.02 μM。KR-39038 通过抑制 HDAC5 通路，明显抑制血管紧张素 II 诱导的新生儿心肌细胞肥大。
储存条件
2-8°C储存,充氩,干燥
运输条件
低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
475.00
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 115 mg/mL (242.11 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于2–8 °C、氩气保护、干燥条件下保存。本品在氩气保护下供应，每次取用后请在惰性气体下重新密封。
本产品如何运输？
本产品采用湿冰冷藏运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2770300-35-9，分子式为 C24H32ClFN6O，分子量为 475.00 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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