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Nesuparib

Cat. No. M29141
Nesuparib Structure
Synonym:

JPI-547/OCN-201

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Biological Activity

Nesuparib is a potent inhibitor of PARP. Nesuparib is useful for the research of neuropathic pain, neurodegenerative disease, and cardiovascular disease.

Chemical Information
Molecular Weight 400.48
Formula C23H24N6O
CAS Number 2055357-64-5
Form Solid
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Xin-Mei Li, et al. Cancer Chemother Pharmacol. Absorption, distribution, metabolism, and excretion of [14C]Mefuparib (CVL218), a novel PARP1/2 inhibitor, in rats

[2] Sali Abubaker Bagabir, et al. J Infect Public Health. Covid-19 and Artificial Intelligence: Genome sequencing, drug development and vaccine discovery

[3] Sorin Avram, et al. Nucleic Acids Res. DrugCentral 2021 supports drug discovery and repositioning

[4] Di Nie, et al. Nano Lett. Cancer-Cell-Membrane-Coated Nanoparticles with a Yolk-Shell Structure Augment Cancer Chemotherapy

[5] Jin-Xue He, et al. Oncotarget. Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution

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Keywords: Nesuparib, JPI-547/OCN-201 supplier, PARP, inhibitors, activators


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