Synonym
DR2313; DR 2313; DR-2313; PARP Inhibitor XI
IUPAC/Chemical Name
3,5,7,8-tetrahydro-2-methyl-4H-thiopyrano[4,3-d]pyrimidin-4-one
InChi Key
HRYKZAKEAVZGJD-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H10N2OS/c1-5-9-7-2-3-12-4-6(7)8(11)10-5/h2-4H2,1H3,(H,9,10,11)
SMILES Code
O=C(N=C(C)N1)C2=C1CCSC2
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
DR2313 is an inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively.
In vitro activity:
In in vitro models of cerebral ischemia, exposure to hydrogen peroxide or glutamate induced cell death with overactivation of PARP, and treatment with DR2313 reduced excessive formation of poly(ADP-ribose) and cell death.
Reference: J Pharmacol Exp Ther. 2005 Feb;312(2):472-81. https://pubmed.ncbi.nlm.nih.gov/15466246/
In vivo activity:
In both permanent and transient focal ischemia models in rats, pretreatment with DR2313 (10 mg/kg i.v. bolus and 10 mg/kg/h i.v. infusion for 6 h) significantly reduced the cortical infarct volume. These results indicate that DR2313 exerts neuroprotective effects via its potent PARP inhibition, even when the treatment is initiated after ischemia.
Reference: J Pharmacol Exp Ther. 2005 Feb;312(2):472-81. https://pubmed.ncbi.nlm.nih.gov/15466246/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
10.0 |
0.55 |
| DMSO |
16.8 |
92.37 |
| Ethanol |
3.5 |
19.21 |
| PBS (pH 7.2) |
0.3 |
1.65 |
| Water |
68.0 |
373.13 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
182.24
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Nakajima H, Kakui N, Ohkuma K, Ishikawa M, Hasegawa T. 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. Epub 2004 Oct 1. PMID: 15466246.
In vitro protocol:
1. Nakajima H, Kakui N, Ohkuma K, Ishikawa M, Hasegawa T. 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. Epub 2004 Oct 1. PMID: 15466246.
In vivo protocol:
1. Nakajima H, Kakui N, Ohkuma K, Ishikawa M, Hasegawa T. 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. Epub 2004 Oct 1. PMID: 15466246.
1. Nakajima, H., Kakuki, N., Ohkuma, K., 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. 312(2), 472-481 (2005).
2. Xu, Z., Zhang, J., David, K.K., 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. 299(1), R215-R221 (2010).
