2. GPCR/G Protein Epigenetics Cell Cycle/DNA Damage
  3. G Protein-coupled Receptor Kinase (GRK) HDAC
  4. KR-39038

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。

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KR-39038 Chemical Structure

KR-39038 Chemical Structure

CAS No. : 2770300-35-9

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5 mg ￥5000
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Customer Review

KR-39038 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KR-39038 相关抗体:

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].

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

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)[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.
分子量

475.00

Formula

C24H32ClFN6O
CAS 号
性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

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

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 115 mg/mL (242.11 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : 100 mg/mL (210.53 mM; 超声助溶 (<80°C))

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

KR-39038 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.1053 mL 10.5263 mL 21.0526 mL 52.6316 mL
5 mM 0.4211 mL 2.1053 mL 4.2105 mL 10.5263 mL
10 mM 0.2105 mL 1.0526 mL 2.1053 mL 5.2632 mL
15 mM 0.1404 mL 0.7018 mL 1.4035 mL 3.5088 mL
20 mM 0.1053 mL 0.5263 mL 1.0526 mL 2.6316 mL
25 mM 0.0842 mL 0.4211 mL 0.8421 mL 2.1053 mL
30 mM 0.0702 mL 0.3509 mL 0.7018 mL 1.7544 mL
40 mM 0.0526 mL 0.2632 mL 0.5263 mL 1.3158 mL
50 mM 0.0421 mL 0.2105 mL 0.4211 mL 1.0526 mL
60 mM 0.0351 mL 0.1754 mL 0.3509 mL 0.8772 mL
80 mM 0.0263 mL 0.1316 mL 0.2632 mL 0.6579 mL
100 mM 0.0211 mL 0.1053 mL 0.2105 mL 0.5263 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KR-390382770300-35-9KR39038KR 39038G Protein-coupled Receptor Kinase (GRK)HDACHistone deacetylasesHypertrophyHeart failureanti-hypertrophiccardioprotectiveneonatal cardiomyocytesorally activeInhibitorinhibitorinhibit

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