KR-32568

Names

[ Name ]:
KR-32568

[Synonym ]:
[5-(2-Methyl-5-fluorophenyl)furan-2-ylcarbonyl]guanidine

Biological Activity

[Description]:

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

[Related Catalog]:

Research Areas >> Cardiovascular Disease

[Target]

IC50: 230 nM (NHE-1)[2]

[In Vitro]

KR-32568 (10 nM-1 μM) 以浓度依赖性方式抑制 NHE-1 介导的兔富血小板血浆细胞内酸化引起的血小板肿胀，IC50 值为 24 nM[1]。

[In Vivo]

KR-32568（0.1-1.0 mg/kg；i.v.；一次）对大鼠发挥有效的心脏保护作用，例如减少梗塞面积，并显着减少室性早搏的总数[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.

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.38g/cm3

[ Boiling Point ]:
444.1ºC at 760 mmHg

[ Molecular Formula ]:
C₁₃H₁₂FN₃O₂

[ Molecular Weight ]:
261.25200

[ Flash Point ]:
222.4ºC

[ Exact Mass ]:
261.09100

[ PSA ]:
92.11000

[ LogP ]:
3.20830

[ Index of Refraction ]:
1.617

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
Eyeshields;Faceshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Carbonic anhydrase activation is associated with worsened pathological remodeling in human ischemic diabetic cardiomyopathy.

J. Am. Heart Assoc. 3(2) , e000434, (2014)

Diabetes mellitus (DM) has multifactorial detrimental effects on myocardial tissue. Recently, carbonic anhydrases (CAs) have been shown to play a major role in diabetic microangiopathy but their role ...