KR-39038 - ≥98% , CAS No.2770300-35-9

CAS: 2770300-35-9 Cat. No.: K650114 Formula: C₂₄H₃₂ClFN₆O Peso molecolare: 475.00

GRADE & PURITY ≥98%

Storage

Store at 2-8°C,Argon charged,Desiccated

Shipped In

Wet ice

Panoramica

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

Specifications

Specifiche e purezza

≥98%

Meccanismi biochimici e fisiologici

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 cardiomyoc

Condizioni di conservazione di stoccaggio

Store at 2-8°C,Argon charged,Desiccated

Spedito in

Wet ice

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Purezza

≥98%

Nomi e identificatori

• Peso molecolare: 475.00

Proprietà chimiche e fisiche

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

Domande frequenti

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at 2–8 °C, desiccated, under argon. It is supplied under an argon blanket; reseal under inert gas after each use.

How is this product shipped?

This product ships chilled on wet ice. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2770300-35-9, the molecular formula is C24H32ClFN6O, and the molecular weight is 475.00 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.