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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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03492177||Recruiting||Drug: selexipag (Uptravi)||Pulmonary Arterial Hypertension||Actelion||July 25 2018||Phase 2|
|NCT03496506||Completed||Drug: Selexipag|Drug: Clopidogrel||Healthy Subjects||Actelion||March 5 2018||Phase 1|
|NCT02791815||Completed||Drug: Midazolam|Drug: Selexipag||Healthy Subjects||Actelion||July 2016||Phase 1|
|NCT02770222||Completed||Drug: Selexipag|Drug: Gemfibrozil|Drug: Rifampicin||Healthy Subjects||Actelion||June 2016||Phase 1|
|NCT02206295||Completed||Drug: selexipag||Bioequivalence||Actelion||September 2012||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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