EB 47

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Cat.No. 4140 - EB 47 | C24H27N9O6.2HCl | CAS No. 1190332-25-2
Description: Potent PARP-1 inhibitor
Chemical Name: 5'-Deoxy-5'-[4-[2-[(2,3-Dihydro-1-oxo-1H-isoindol-4-yl)amino]-2-oxoethyl]-1-piperazinyl]-5'-oxoadenosine dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Reviews
Literature

Biological Activity

Potent inhibitor of PARP-1 (IC50 = 45 nM). Reduces infarct volume in both a rat transient middle cerebral arterial occlusion model and a cardiac reperfusion model.

Compound Libraries

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Technical Data

M. Wt 610.45
Formula C24H27N9O6.2HCl
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1190332-25-2
PubChem ID 90488915
InChI Key VVMQSDIMNDTMII-GWZGOYLNSA-N
Smiles O=C(NC2=CC=CC3=C2CNC3=O)CN(CC1)CCN1[C@]([C@@H]4O[C@H](N5C=NC6=C5N=CN=C6N)[C@@H](O)[C@H]4O)=O.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 3.05 5 with gentle warming
DMSO 30.52 50

Preparing Stock Solutions

The following data is based on the product molecular weight 610.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 3.28 mL 16.38 mL 32.76 mL
2.5 mM 0.66 mL 3.28 mL 6.55 mL
5 mM 0.33 mL 1.64 mL 3.28 mL
25 mM 0.07 mL 0.33 mL 0.66 mL

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References

References are publications that support the biological activity of the product.

Jagtap et al (2004) The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1). Bioorg.Med.Chem.Lett. 14 81 PMID: 14684303

Ferraris et al (2010) Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic. J.Med.Chem. 53 4561 PMID: 20364863

Gaymes et al (2009) Inhibitors of poly ADP-ribose polymerase (PARP) induce apoptosis of myeloid leukemic cells: potential for therapy of myeloid leukemia and myelodysplastic syndromes. Haematologica 94 638 PMID: 19407318


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Keywords: EB 47, EB 47 supplier, EB47, PARP-1, poly(ADP-ribose), polymerase-1, inhibitors, inhibits, PARP1, Poly(ADP-ribose), Polymerase, 4140, Tocris Bioscience

3 Citations for EB 47

Citations are publications that use Tocris products. Selected citations for EB 47 include:

Rom et al (2016) PARP inhibition in leukocytes diminishes inflammation via effects on integrins/cytoskeleton and protects the blood-brain barrier Journal of Neuroinflammation 13 254 PMID: 27677851

Rom et al (2015) Poly(ADP-ribose) polymerase-1 inhibition in brain endothelium protects the blood-brain barrier under physiologic and neuroinflammatory conditions. Front Microbiol 35 28 PMID: 25248836

Rom et al (2015) The dual action of poly(ADP-ribose) polymerase -1 (PARP-1) inhibition in HIV-1 infection: HIV-1 LTR inhibition and diminution in Rho GTPase activity. Dev Biol 6 878 PMID: 26379653


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Literature in this Area

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