1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. KCL-440

KCL-440 

Cat. No.: HY-15050
Handling Instructions

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

For research use only. We do not sell to patients.

KCL-440 Chemical Structure

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].

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.
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Storage

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

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KCL-440
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HY-15050
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