| Identification | Back Directory | [Name]
1,5,7,8-TETRAHYDRO-2-METHYL-4H-THIOPYRANO[4,3-D]PYRIMIDIN-4-ONE | [CAS]
284028-90-6 | [Synonyms]
DR 2313
IR 2313
SC-202756
DR2313 >=98% (HPLC)
PARP Inhibitor XI, DR2313
4H-Thiopyrano[4,3-d]pyriMidin-4-one,3,5,7,8-tetrahydro-2
7,8-Dihydro-2-methyl-1H-thiopyrano[4,3-d]pyrimidin-4(5H)-one
3,5,7,8-Tetrahydro-2-methyl-4H-thiopyrano[4,3-d]pyrimidin-4-one
1,5,7,8-TETRAHYDRO-2-METHYL-4H-THIOPYRANO[4,3-D]PYRIMIDIN-4-ONE
2-Methyl-1-sulfanyl-1H,4H,5H,7H,8H-pyrano[4,3-d]pyriMidin-4-one
4H-THIOPYRANO[4,3-D]PYRIMIDIN-4-ONE,3,5,7,8-TETRAHYDRO-2-METHYL-
3,5,7,8-tetrahydro-2-methyl-4h-thiopyrano(4,3-d)pyrimidin-4-one, 98%(HPLC) | [EINECS(EC#)]
200-589-5 | [Molecular Formula]
C8H10N2OS | [MDL Number]
MFCD08703132 | [MOL File]
284028-90-6.mol | [Molecular Weight]
182.24 |
| Chemical Properties | Back Directory | [Boiling point ]
349.3±52.0 °C(Predicted) | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
H2O: >2mg/mL (warmed) | [form ]
powder | [pka]
1.54±0.20(Predicted) | [color ]
white to beige | [Water Solubility ]
H2O: >2mg/mL (warmed) | [InChI]
1S/C8H10N2OS/c1-5-9-7-2-3-12-4-6(7)8(11)10-5/h2-4H2,1H3,(H,9,10,11) | [InChIKey]
HRYKZAKEAVZGJD-UHFFFAOYSA-N | [SMILES]
CC1=NC(=O)C2=C(CCSC2)N1 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Potent, competitive inhibitor of poly(ADP-ribose) polymerase (PARP) (IC 50 values are 0.20 and 0.24 μ M for PARP-1 and PARP-2 respectively). Neuroprotective; reduces neuronal cell death in models of cerebral ischemia in vivo and in vitro . Brain penetrant. | [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].
| 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. |
| [IC 50]
PARP-1: 0.20 μM (IC50); PARP-2: 0.24 μM (IC50) | [References]
[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. DOI:10.1124/jpet.104.075465
[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. DOI:10.1152/ajpregu.00747.2009 |
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