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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.
| 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 | 473.51 |
| Formula | C25H22F3NO3S |
| CAS Number | 1006036-87-8 |
| Purity | >98% |
| Solubility | DMSO ≥ 20 mg/mL |
| Storage | at -20°C |
| Related Prostaglandin Receptor Products |
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| MF-766
MF-766 is a highly effective, selective and orally active EP4 antagonist.Ki The value is 0.23 nM. MF-766 behaves as a complete antagonist with its IC in functional detection50 1.4 nM (becomes 1.8 nM when 10% HS is present). MF-766 can be used for cancer and inflammatory disease research. |
| MF498
MF498 is a novel selective prostaglandin E4 receptor (EP4 receptor) antagonist with a strong affinity with the EP4 receptor, with a Ki of 0.7 nM. |
| KAG-308
KAG-308 is an effective, selective, orallyable EP4 receptor (a subtype of prostaglandin E2 receptor) agonist that inhibits colitis, promotes tissue mucosal healing, and effectively inhibits the production of TNF-α. KAG-308 for human EP4 receptors Ki value and EC50 The values were 2.57 nM and 17 nM, respectively, which were more selective than EP1, EP2, EP3, and IP receptors. |
| GSK726701A
GSK726701A is a partial agonist of prostaglandin E2 receptor 4 (EP4),pEC50is 7.4. |
| CJ-42794
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. |
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