製品番号: HY-143248

KR-39038

1 Cited Publications

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.68%
CAS 番号: 2770300-35-9
分子式: C₂₄H₃₂ClFN₆O
分子量:475.00

保管条件:

4°C, stored under nitrogen

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

KR-39038 構造式

CAS 番号: 2770300-35-9

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

HDAC5

HDAC アイソフォーム固有の製品をすべて表示 :

体外実験

KR-39038 (0-1.0 μM, 24 h) significantly inhibits angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes^[1].

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

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.

体内実験

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)
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

MedChemExpress (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.

化学情報

CAS 番号 2770300-35-9
性状 Solid
分子量 475.00
分子式 C₂₄H₃₂ClFN₆O
Color White to yellow
SMILES

O=C1N=C(C2=C(Cl)C=CC=C2)NC3=CC(NCCCNCCCCNCCCN)=C(C=C13)F
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, stored under nitrogen

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

Publications (1)

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Journal Impact Factor

Commun Biol

Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation. [Abstract]

2026 Jan 16;9(1):287. PMID: 41545717

溶剤 & 溶解度

体外:

DMSO : 115 mg/mL (242.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (210.53 mM; ultrasonic and warming and heat to 80°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

KR-39038

1 Cited Publications

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KR-39038

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

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Kinase Inhibitor Library

Histone Modification Research Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

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Anti-Breast Cancer Compound Library

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Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

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MCE Bioactive Compound Library

Bioactive Compound Library

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Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 KR-39038

HDAC アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

KR-39038

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Histone Modification Research Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 KR-39038

HDAC アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

KR-39038 関連分類

製品番号: HY-143248