DR 2313

CAS No. 284028-90-6

DR 2313( —— )

Catalog No. M24196 CAS No. 284028-90-6

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).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    DR 2313
  • Note
    Research use only, not for human use.
  • Brief 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).
  • 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.
  • 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.
  • 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 ischemiaResult:Reduced the infarct volume in a dose-dependent manner in pMCAo and tMCAo model.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP1|PARP2
  • Research Area
    ——
  • Indication
    ——

Chemical Information

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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Nakajima H, et, al. A newly synthesized poly(ADP-ribose) polymerase inhibitor, DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: pharmacological profiles, neuroprotective effects, and therapeutic time window in cerebral ischemia in rats. J Pharmacol Exp Ther. 2005 Feb;312(2):472-81.
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