KCL-440

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KCL-440 is a CNS-penetrated PARP inhibitor, with an IC₅₀ of 68 nM. KCL-440 has strong inhibition of PARP-1.

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KCL-440 Chemical Structure

CAS No. : 651029-09-3

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Description

KCL-440 is a CNS-penetrated PARP inhibitor, with an IC₅₀ of 68 nM. KCL-440 has strong inhibition of PARP-1^[1]^[2].

IC₅₀ & Target

IC50: 68 nM (PARP)^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

294.35

Formula

C₁₈H₁₈N₂O₂

CAS No.

651029-09-3

SMILES

O=C1NC=C(C2=CC=C(CN(C)C)C=C2)C3=C(O)C=CC=C31

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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.

KCL-440 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KCL-440651029-09-3KCL440KCL 440PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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