DR 2313

SKU: orb1218227

Description

DR 2313 is a competitive inhibitor of poly(ADP-ribose) polymerase (IC50: 0.20 and 0.24 μM for PARP-1 and PARP-2 respectively). It also has neuroprotective.

Key Properties

• CAS Number: 284028-90-6
• MW: 182.24
• Purity: >98% (HPLC)
• Formula: C₈H₁₀N₂OS
• SMILES: O=C(N=C(C)N1)C2=C1CCSC2
• Target: PARP
• Solubility: DMSO:83.3mg/mL;H2O:9.1mg/mL

Bioactivity

• 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. Animal model: Male Wistar rats (220-300 g) with permanent MCA occlusions (pMCAos) and transient MCA occlusions (tMCAos). 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.
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• 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. 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). DR2313 (1-100 μM; 10 min) shows a weak inhibition of the mono(ADP-ribosyl)ation in a concentration-dependent manner (IC50 = 59 μM). 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PARP