KR-39038

• CAT Number: I043449
• CAS Number: 2770300-35-9
• Purity: ≥95%
• Synonyms: 7-[3-[4-(3-aminopropylamino)butylamino]propylamino]-2-(2-chlorophenyl)-6-fluoro-3H-quinazolin-4-one
• InChI: InChI=1S/C24H32ClFN6O/c25-19-8-2-1-7-17(19)23-31-21-16-22(20(26)15-18(21)24(33)32-23)30-14-6-13-29-11-4-3-10-28-12-5-9-27/h1-2,7-8,15-16,28-30H,3-6,9-14,27H2,(H,31,32,33)
• InChIKey: UEAYNKFJXGVWBQ-UHFFFAOYSA-N
• SMILES: C1=CC=C(C(=C1)C2=NC3=CC(=C(C=C3C(=O)N2)F)NCCCNCCCCNCCCN)Cl

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