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DG-041 is an antagonist of high affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively ). DG-041 inhibits PGE2 facilitation of platelet aggregation and it also crosses the blood-brain barrier.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $43 | In Stock | |
2 mg | $61 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $162 | In Stock | |
25 mg | $316 | In Stock | |
50 mg | $568 | In Stock | |
100 mg | $818 | In Stock | |
500 mg | $1,690 | In Stock | |
1 mL x 10 mM (in DMSO) | $112 | In Stock |
Description | DG-041 is an antagonist of high-affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively). DG-041 inhibits PGE2 facilitation of platelet aggregation and has the blood-brain barrier permeability. |
Targets&IC50 | EP3 receptor:4.6/8.1 nM |
In vitro | DG-041 was a less effective the DP1 (IC50: 131 nM), EP1 (IC50: 486 nM) and TP receptors (IC50: 742 nM) antagonist [1]. |
In vivo | DG-041 has CL of 1250 mL/h/kg for intravenous. DG-041 (1.78 mg/kg for i.v or 9.62 mg/kg for p.o) has t1/2 of 2.7 hours, 4.06 hours. DG-041 (1.78 mg/kg for i.v or 9.62 mg/kg for p.o) has Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively [1]. |
Molecular Weight | 592.32 |
Formula | C23H15Cl4FN2O3S2 |
Cas No. | 861238-35-9 |
Smiles | Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(\C=C\C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 |
Relative Density. | 1.57 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/ml (92.86 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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