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

KCL-440 是能透过中枢神经系统的 PARP 抑制剂，其 IC50 值为 68 nM。KCL-440 对 PARP-1 有很强的抑制活性。

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KCL-440 Chemical Structure

KCL-440 Chemical Structure

CAS No. : 651029-09-3

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KCL-440 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].
体内研究
(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.
分子量

294.35

Formula

C18H18N2O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

KCL-440 相关分类

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Keywords:

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

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产品名称：
KCL-440
目录号：
HY-15050
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