ChemicalBook CAS DataBase List 852146-73-7

852146-73-7

Name	KR-32568
CAS	852146-73-7
Molecular Formula	C13H12FN3O2
MDL Number	MFCD08705324
Molecular Weight	261.25
MOL File	852146-73-7.mol

Chemical Properties

Melting point	176 °C
density	1.38±0.1 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO: ~10 mg/mL
form	solid
pka	7.31±0.46(Predicted)
color	white
InChI	1S/C13H12FN3O2/c1-7-2-3-8(14)6-9(7)10-4-5-11(19-10)12(18)17-13(15)16/h2-6H,1H3,(H4,15,16,17,18)
InChIKey	DTLDHYBZLVASJQ-UHFFFAOYSA-N
SMILES	Cc1ccc(F)cc1-c2ccc(o2)C(=O)NC(N)=N

Safety Data

Hazard Codes	Xn
Risk Statements	22-36/37/38 less more
Safety Statements	26-36 less more
WGK Germany	3
Storage Class	10 - Combustible liquids
Hazard Classifications	Acute Tox. 4 Oral Eye Irrit. 2 Skin Irrit. 2 STOT SE 3

Hazard Information

Uses

KR-32568 is a sodium/hydrogen exchanger-1 (NHE-1) inhibitor with an IC50 of 230 nM. KR-32568 has cardioprotective effects[1][2].

Biological Activity

Sodium/hydrogen exchanger-1 (NHE-1) inhibitor; IC50 = 0.23 μM; inhibited NHE-1-mediated rabbit platelet swelling; in anesthetized ratsreduced infarct size from 67% (control) to 43% ( at 0.1 mg/kg) and 24% ( at 1.0 mg/kg); reduced number of ventricular premature beats from 530 to 266 ( at 0.1 mg/kg) and 115 ( at 1.0 mg/kg); reduced ventricular fibrillation incidence from 17 to 8 (0.1 mg/kg) and 0 (1.0 mg/kg); implications for research and treatment of myocardial ischemic diseases.

in vivo

KR-32568 (0.1-1.0 mg/kg; i.v.; once) exert potent cardioprotective effects in rats, such as reduces infarct size, and significantly reduces the total number of ventricular premature beats^[1].

Animal Model:	Male Sprague-Dawley rats (350-380 g) bearing 30 min ischemia/2.5 h reperfusion heart injury^[1]
Dosage:	0.1 mg/kg and 1.0 mg/kg
Administration:	i.v.; once
Result:	Exerted potent cardioprotective effects in rats.

storage

Store at -20°C

References

[1] Hui-Yul Roh, et al. Cardioprotective effects of [5-(2-methyl-5-fluorophenyl)furan-2-ylcarbonyl]guanidine (KR-32568) in an anesthetized rat model of ischemia and reperfusion heart injury. Pharmacology. 2005 Dec;75(1):37-44. DOI:10.1159/000086192
[2] Sunkyung Lee, et al. (5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1. J Med Chem. 2005 Apr 21;48(8):2882-91. DOI:10.1021/jm0492305

Spectrum Detail

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