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Cat. No.: HY-15050

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KCL-440

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.

CAS No.: 651029-09-3
Formula: C₁₈H₁₈N₂O₂
Molecular Weight:294.35

Storage:

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

Data Sheet (271 KB)

KCL-440 Chemical Structure

CAS No.: 651029-09-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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].

All PARP Isoforms :

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.

Chemical Information

CAS No. 651029-09-3
Molecular Weight 294.35
Formula C₁₈H₁₈N₂O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References

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KCL-440

All PARP Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

KCL-440 Related Classifications

HY-15050 Related Classifications