| Bioactivity | DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier[1][2]. | ||||||||||||
| Invitro | DG-041 was a less potent antagonist of the DP1 (IC50=131 nM), EP1 (IC50=486 nM), and TP receptors (IC50=742 nM)[1]. | ||||||||||||
| In Vivo | DG-041 (1.78 mg/kg for intravenous or 9.62 mg/kg for oral) has t1/2 of 2.7 hours, 4.06 hours and Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively. DG-041 has CL of 1250 mL/h/kg for intravenous[1]. Animal Model: | ||||||||||||
| Name | DG-041 | ||||||||||||
| CAS | 861238-35-9 | ||||||||||||
| Formula | C23H15Cl4FN2O3S2 | ||||||||||||
| Molar Mass | 592.32 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Singh J, et al. Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding. ACS Chem Biol. 2009 Feb 20;4(2):115-26. [2]. Hategan G, et al. Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptorantagonists. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6797-800. |
DG-041
CAS: 861238-35-9 F: C23H15Cl4FN2O3S2 W: 592.32
DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding a
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