DR2313
Based on 1 Customer Validation
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.
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- Pureté: 99.66%
- CAS No.: 284028-90-6
- Formule: C8H10N2OS
- Masse moléculaire:182.25
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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PARP-1 0.20 μM (IC50) |
PARP-2 0.24 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (220-300 g) with permanent MCA occlusions (pMCAos) and transient MCA occlusions (tMCAos)[1]
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Dosage:3, 10 mg/kg
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Administration:I.v. bolus and i.v. infusion for 6 h beginning 5 min before the onset of ischemia
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Result:Reduced the infarct volume in a dose-dependent manner in pMCAo and tMCAo model.
Chemical Information
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CAS No. 284028-90-6
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Appearance Solid
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Masse moléculaire 182.25
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Formule C8H10N2OS
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Color White to off-white
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SMILES
O=C1C(CSCC2)=C2NC(C)=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
H2O : ≥ 100 mg/mL (548.70 mM)
DMSO : 12.5 mg/mL (68.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[2]. Xu Z, et, al. Endonuclease G does not play an obligatory role in poly(ADP-ribose) polymerase-dependent cell death after transient focal cerebral ischemia. Am J Physiol Regul Integr Comp Physiol. 2010 Jul;299(1):R215-21. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 5.4870 mL | 27.4351 mL | 54.8703 mL | 137.1757 mL |
| 5 mM | 1.0974 mL | 5.4870 mL | 10.9741 mL | 27.4351 mL | |
| 10 mM | 0.5487 mL | 2.7435 mL | 5.4870 mL | 13.7176 mL | |
| 15 mM | 0.3658 mL | 1.8290 mL | 3.6580 mL | 9.1450 mL | |
| 20 mM | 0.2744 mL | 1.3718 mL | 2.7435 mL | 6.8588 mL | |
| 25 mM | 0.2195 mL | 1.0974 mL | 2.1948 mL | 5.4870 mL | |
| 30 mM | 0.1829 mL | 0.9145 mL | 1.8290 mL | 4.5725 mL | |
| 40 mM | 0.1372 mL | 0.6859 mL | 1.3718 mL | 3.4294 mL | |
| 50 mM | 0.1097 mL | 0.5487 mL | 1.0974 mL | 2.7435 mL | |
| 60 mM | 0.0915 mL | 0.4573 mL | 0.9145 mL | 2.2863 mL | |
| H2O | 80 mM | 0.0686 mL | 0.3429 mL | 0.6859 mL | 1.7147 mL |
| 100 mM | 0.0549 mL | 0.2744 mL | 0.5487 mL | 1.3718 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
DR2313 Related Classifications
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