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

KR-39038 

Cat. No.: HY-143248 Purity: 98.65%
Handling Instructions

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.

For research use only. We do not sell to patients.

KR-39038 Chemical Structure

KR-39038 Chemical Structure

CAS No. : 2770300-35-9

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Description

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

 

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.

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.
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.
Molecular Weight

475.00

Formula

C24H32ClFN6O

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 115 mg/mL (242.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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