Molecular Weight(MW): 419.52
MRE-269(ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.
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|Description||MRE-269(ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.|
MRE-269 bound to the human IP receptor with high affinity (binding affinity (Ki) of 20 nM) and with more than 130-fold selectivity over other prostanoid receptors (prostaglandin E receptors, EP1−4; prostaglandin D receptor, DP1; prostaglandin F2 receptor, FP; thromboxane A2 receptor, TP). In pulmonary arterial smooth muscle cells (PASMCs), MRE-269 potently induces accumulation of intracellular cAMP, leading to long-lasting (>10 h) membrane hyperpolarization (EC50 = 32 nM) which contributes to cell relaxation. It also causes long-lasting and pronounced relaxation of PASMCs.
|In vivo||After Oral Administration (1 mg/kg) to monkeys, the Tmax (time to reach maximum observed plasma concentration), Cmax (maximum observed plasma concentration), AUC0−24h (area under the curve from 0 to 24 h after dosing) and T1/2 (apparent terminal half-life) are 2.3 h, 105 ng/mL, 652 ng·h/mL and 5.6 h, respectively for MRE-269.|
|In vitro||DMSO||84 mg/mL (200.22 mM)|
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