| Identification | Back Directory | [Name]
KR-32568 | [CAS]
852146-73-7 | [Synonyms]
KR 32568,KR32568
KR-32568 >=98% (HPLC), solid
2-Furancarboxamide, N-(aminoiminomethyl)-5-(5-fluoro-2-methylphenyl)- | [Molecular Formula]
C13H12FN3O2 | [MDL Number]
MFCD08705324 | [MOL File]
852146-73-7.mol | [Molecular Weight]
261.25 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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Merck KGaA
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