1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. DR2313

DR2313 

Cat. No.: HY-105692
Handling Instructions

DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo.

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

DR2313 Chemical Structure

DR2313 Chemical Structure

CAS No. : 284028-90-6

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Description

DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo[1][2].

IC50 & Target[1]

PARP-1

0.20 μM (IC50)

PARP-2

0.24 μM (IC50)

In Vitro

DR2313 (0.016-16.4 μM; 30 min) inhibits poly(ADP-ribosyl)ation reaction in nuclear extracts of rat brain, with a Ki of 0.23 μM[1].
DR2313 shows more powerful inhibition of the poly(ADP-ribosyl)ation in the nuclear extracts of the rat brain (IC50=0.20 μM) than 3AB (35.4 μM), PND (0.56 μM), DIQ (2.96 μM), and DPQ (0.96 μM)[1].
DR2313 (1-100 μM; 10 min) shows a weak inhibition of the mono(ADP-ribosyl)ation in a concentration-dependent manner (IC50=59 μM)[1].
DR2313 (0.1-30 μM; pretreated for 30 min) reduces hydrogen peroxide (500 μM; 4 h) or glutamate (1 mM; 30 min) induced excessive formation of poly(ADP-ribose) and cell death[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

DR2313 (3-10 mg/kg i.v. bolus or infusion for 6 h) significantly reduces the cortical infarct volume in both permanent and transient focal ischemia models in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (220-300 g) with permanent MCA occlusions (pMCAos) and transient MCA occlusions (tMCAos)[1]
Dosage: 3, 10 mg/kg
Administration: I.v. bolus and i.v. infusion for 6 h beginning 5 min before the onset of ischemia
Result: Reduced the infarct volume in a dose-dependent manner in pMCAo and tMCAo model.
Molecular Weight

182.24

Formula

C₈H₁₀N₂OS

CAS No.
SMILES

O=C1C(CSCC2)=C2NC(C)=N1

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

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Keywords:

DR2313DR 2313DR-2313PARPpoly ADP ribose polymerasepoly(ADP-ribose)polymeraseneuroprotectiveischemicInhibitorinhibitorinhibit

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