L-902688 is a potent, selective and orally active EP4 receptor agonist with a Ki of 0.38 nM and an EC50 of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors.
| Molecular Weight | 419.47 |
| Formula | C21H27F2N5O2 |
| CAS Number | 634193-54-7 |
| Form | Liquid |
| Storage | -20°C |
| 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.
[4] A W Cuthbert. Br J Pharmacol. Lubiprostone targets prostanoid EP₄ receptors in ovine airways
| 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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