TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels. TG4-155 crosses the blood brain barrier, and has no antagonistic effects on EP4 signaling, and displays neuroprotective effects in a pilocarpine-induced status epilepticus (SE) seizure model. TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine.
|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: ≥ 25 mg/mL|
Prostanoid receptor EP2 as a therapeutic target.
Ganesh T. J Med Chem. 2014 Jun 12;57(11):4454-65. PMID: 24279689.
Role of prostaglandin receptor EP2 in the regulations of cancer cell proliferation, invasion, and inflammation.
Jiang J, et al. J Pharmacol Exp Ther. 2013 Feb;344(2):360-7. PMID: 23192657.
|Related Prostaglandin Receptor Products|
Dinoprost tromethamine (Prostaglandin F2α tromethamine) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist.
Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM.
Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.
GW627368X is a novel, potent and selective competitive antagonist of prostanoid EP4 receptors with additional human TP receptor affinity.
Taprenepag, also known as CP-544326, is a potent and selective EP(2) receptor agonist, with IC50 values of 10 and 15 nM for human and rat EP2, respectively.
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