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DR2313

Cat. No. M8325
DR2313 Structure
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Biological Activity

DR2313 is a PARP-1; PARP-2 inhibitor (Ki = 0.23 mM). DR2313 has neuroprotective effects in both in vivo and in vitro ischemic models, and reduces cortical infarct volume in focal ischemia in rats.

Chemical Information
Molecular Weight 182.24
Formula C8H10N2OS
CAS Number 284028-90-6
Solubility (25°C) Water: ≥2 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Wei Qiu, et al. Insights into the binding of PARP inhibitors to the catalytic domain of human tankyrase-2

[2] Hidemitsu Nakajima, 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

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Keywords: DR2313 supplier, inhibitors, activators


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