DG-041

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DG-041 是高亲和力 EP3 受体的拮抗剂（IC50：在结合和 FLIPR 测定中分别为 4.6 nM 和 8.1 nM）。

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.(In Vitro):DG-041 was a less effective the DP1 (IC50=131 nM), EP1 (IC50=486 nM) and TP receptors (IC50=742 nM) antagonist.(In Vivo):DG-041 has CL of 1250 mL/h/kg for intravenous. 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. DG-041 (1.78 mg/kg for intravenous or 9.62 mg/kg for oral) has Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively .

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Animal Model:Male Sprague Dawley rat Dosage:1.78 mg/kg (intravenous) or 9.62 mg/kg (oral) Administration:Intravenous or oral Result:Had t1/2 of 2.7 hours, 4.06 hours and Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively.

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GPCR/G Protein

Prostaglandin Receptor

NR1A| NR2B-NMDA

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861238-35-9

592.3

C23H15Cl4FN2O3S2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (422.07 mM)

Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(\C=C\C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12

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(-20℃)

With Ice Pack

≥ 2 years