Home GPCR & G Protein Prostaglandin Receptor agonist MRE-269 (ACT-333679) For research use only.

MRE-269 (ACT-333679)

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 (ACT-333679) Chemical Structure

MRE-269 (ACT-333679) Chemical Structure

CAS No. 475085-57-5

Purity & Quality Control

Batch: S581901 DMSO]84 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.93%
99.93

MRE-269 (ACT-333679) Related Products

Biological Activity

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.
Targets
human IP receptor [1]
20 nM(Ki)
In vitro
In vitro 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[1].
In Vivo
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[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04175600 Active not recruiting
Hypertension Pulmonary
Actelion
 January 16 2020 Phase 3
NCT03492177 Active not recruiting
Pulmonary Arterial Hypertension
Actelion
 July 23 2018 Phase 2
NCT03496506 Completed
Healthy Subjects
Actelion
 March 5 2018 Phase 1
NCT02791815 Completed
Healthy Subjects
Actelion
 July 2016 Phase 1
NCT02770222 Completed
Healthy Subjects
Actelion
 June 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 419.52 Formula

C25H29N3O3
CAS No. 475085-57-5 SDF --
Smiles CC(C)N(CCCCOCC(=O)O)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (200.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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