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

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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DR2313 Chemical Structure

DR2313 Chemical Structure

CAS No. : 284028-90-6

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Based on 1 publication(s) in Google Scholar

DR2313 Related Antibodies

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View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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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].

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

DR2313 Related Antibodies
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].

MedChemExpress (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

182.25

Formula

C8H10N2OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.4870 mL 27.4351 mL 54.8703 mL
5 mM 1.0974 mL 5.4870 mL 10.9741 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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DR2313 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DR2313284028-90-6DR 2313DR-2313PARPpoly ADP ribose polymerasepoly(ADP-ribose)polymeraseneuroprotectiveischemicInhibitorinhibitorinhibit

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