651029-09-3

Name	KCL 440
CAS	651029-09-3
Molecular Formula	C18H18N2O2
MDL Number	MFCD19443779
Molecular Weight	294.35
MOL File	651029-09-3.mol

Synonyms

KCL 440 RS57639 RS-57639 RS 57639 1(2H)-Isoquinolinone, 4-[4-[(dimethylamino)methyl]phenyl]-5-hydroxy-

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Chemical Properties

Boiling point	512.4±50.0 °C(Predicted)
density	1.230±0.06 g/cm3(Predicted)
pka	8.29±0.20(Predicted)

Hazard Information

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.

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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