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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 60 mg/mL|
 Yasutaka Murahashi, et al. Sci Rep. Oral administration of EP4-selective agonist KAG-308 suppresses mouse knee osteoarthritis development through reduction of chondrocyte hypertrophy and TNF secretion
 Yusuke Watanabe, et al. Eur J Pharmacol. KAG-308, a newly-identified EP4-selective agonist shows efficacy for treating ulcerative colitis and can bring about lower risk of colorectal carcinogenesis by oral administration
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