ONO-AE3-208 is an orally active prostaglandin E2 receptor 4 (EP4)-selective antagonist (Ki in nM = 1.3/EP4, 30/EP3, 790/FP and 2400/TP; Ki >10 μM for prostanoid receptors DP, EP1, EP2, IP). Both EP4-/- mice and ONO-AE3-208-treated wild-type mice (10 mg/kg/day in drinking water) are shown to develop severe symptoms (diarrhea, hemoccult, weight loss) in a murine model of DSS-induced colitis. ONO-AE3-208 is also reported to promote ductus arteriosus constriction among fetal and neonatal rats in vivo (10 mg/kg administered orogastrically). In addition, ONO-AE3-208 is demonstrated to effectively inhibit 1 ng/mL IL-1β-induced HUVEC migration in vitro (53% and 75% inhibition by 1 or 10 μM AE3-208, repectively) and block IL-1β (30 ng/Hydron pellet implant)-induced angionesis in mouse corneas in vivo (1 mg/kg/day p.o.).
| Molecular Weight | 404.43 |
| Formula | C24H21FN2O3 |
| CAS Number | 402473-54-5 |
| Form | Solid |
| Solubility (25°C) | DMSO: 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Prostaglandin Receptor Products |
|---|
| Carbacyclin
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation. |
| DT-9081
DT-9081 is a potentially best-in-class, orally active, small molecule prostaglandin EP4 receptor antagonist that reverses prostaglandin E2 (PGE2)-induced immunosuppression in certain tumors by blocking the EP4 receptor present on immune cells. |
| Unoprostone
Unoprostone is a prostaglandin F2α analog (PGAs) that reduces oxidative stress and light-induced retinal cell death as well as phagocytosis dysfunction by activating BK channels. It can be used in studies related to glaucoma or hypertension. |
| 15-keto-Prostaglandin E2
15-keto-Prostaglandin E2 is an endogenous metabolite. |
| Prostaglandin B1
Prostaglandin B1 (PGB1) is a metabolite of Prostaglandin E1. |
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