| Identification | Back Directory | [Name]
KCL 440 | [CAS]
651029-09-3 | [Synonyms]
KCL 440
RS57639
RS-57639
RS 57639
1(2H)-Isoquinolinone, 4-[4-[(dimethylamino)methyl]phenyl]-5-hydroxy- | [Molecular Formula]
C18H18N2O2 | [MDL Number]
MFCD19443779 | [MOL File]
651029-09-3.mol | [Molecular Weight]
294.35 |
| Hazard Information | Back Directory | [Uses]
KCL-440 is a CNS-penetrated PARP inhibitor, with an IC50 of 68 nM. KCL-440 has strong inhibition of PARP-1[1][2]. | [in vivo]
The brain concentration of KCL-440 is sufficient to inhibit the PARP activity during the intravenous infusion at the rate of 1 mg/kg/h[1].
KCL-440 (over 0.03 mg/kg/h) exhibits neuroprotective effects of KCL-440 in the in vivo cerebral ischemia model[1].
| Animal Model: | Rat acute cerebral infarction model induced by photothrombotic MCA occlusion[1]. | | Dosage: | 0.01, 0.03, 0.1, 0.3, 1.0, and 3.0 mg/kg/h. | | Administration: | Intravenously administered at a rate of 0.33 ml/kg/h for 24 h immediately after
cerebral ischemia.
| | Result: | The serum concentration of KCL-440 approached steadystate levels within 1 h in rats that were intravenously infused at the rate of 1 mg/kg/h for 6 h. One hour after the initiation of infusion, the serum concentration of KCL-440 is 0.11 μg/mL, which is equivalent to 0.37 μM. The brain:serum concentration ratio after a 6-h infusion at 10 mg/kg/h is 0.8.
Led to a dose-dependent reduction in the cerebral infarct size at 24 h after the MCA occlusion.
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| [References]
[1] Yasuhiko Ikeda, et al. Neuroprotective effects of KCL-440, a new poly(ADP-ribose) polymerase inhibitor, in the rat middle cerebral artery occlusion model. Brain Res. 2005 Oct 26;1060(1-2):73-80. DOI:10.1016/j.brainres.2005.08.046
[2] Tatsushi Kamiya, et al. The neuroprotective effects of a newly synthesized poly (ADP-ribose) polymerase (PARP) inhibitor (KCL-440) on neuronal cell death following transient focal ischemia in rat. Journal of Cerebral Blood Flow & Metabolism. 2005. |
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