CJ-42794 is a selective prostaglandin receptor EP4 antagonist that inhibits [3H]-PGE2 binding to EP4 receptors with an average pKi of 8.5 and is more than 200 times more selective than EP1, EP2 and EP3.
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.
Molecular Weight | 413.83 |
Formula | C22H17ClFNO4 |
CAS Number | 847728-01-2 |
Purity | >98% |
Solubility | DMSO ≥ 20 mg/mL |
Storage | at -20°C |
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MK-2894 sodium salt is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). |
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MK-2894
MK-2894 IS AN EFFECTIVE, SELECTIVE, HIGH-AFFINITY (Ki=0.56 nM) of prostaglandin receptor 4 (EP4 receptor) antagonists (IC50=2.5 nM)。 MK-2894 has strong anti-inflammatory activity in animal pain/inflammation models and can be used in arthritis studies. |
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