Size | Price | Stock | Qty |
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10mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
MRE-269 (also known as MRE269; ACT-333679), an active metabolite of selexipag (also known as NS-304), is a novel, potent along-acting and selective IP (prostaglandin I2) receptor agonist. MRE-269 (ACT-333679) possesses a strong binding affinity—130 times higher than that of other human prostanoid receptors—for the human IP receptor.
Targets |
human IP receptor ( Ki = 20 nM )
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ln Vitro |
MRE-269 causes the rat extralobar pulmonary artery (EPA) to vasodilate without the need for endothelium. MRE-269 or other IP receptor agonists including epoprostenol, iloprost, treprostinil and beraprost increase cAMP levels in hPASMC[1]. MRE-269 causes vasodilation in LPA(+), LPA(-), and SPA(-) in response to concentration[3].
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ln Vivo |
MRE-269 exhibits the same vasorelaxant effects on rat small intralobar pulmonary artery (SIPA) and EPA, whereas other IP receptor agonists cause less vasodilation in SIPA compared to EPA[1]. MRE-269 significantly relaxes the rat small pulmonary artery, but its effects don't become noticeable until high concentrations above 10 μM (pEC50, 4.98±0.22). On the other hand, MRE-269 causes only slight relaxation in rat small pulmonary veins across the whole concentration range, with the two highest doses of MRE-269—10 and 100 μM—producing the only notable relaxation[2].
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References |
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Molecular Formula |
C25H29N3O3
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Molecular Weight |
419.5161
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Exact Mass |
419.22
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Elemental Analysis |
C, 71.57; H, 6.97; N, 10.02; O, 11.44
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CAS # |
475085-57-5
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Related CAS # |
MRE-269-d7; 1265295-20-2; MRE-269-d6; 1265295-56-4
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Appearance |
Solid powder
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SMILES |
CC(C)N(CCCCOCC(=O)O)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
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InChi Key |
OJQMKCBWYCWFPU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C25H29N3O3/c1-19(2)28(15-9-10-16-31-18-23(29)30)22-17-26-24(20-11-5-3-6-12-20)25(27-22)21-13-7-4-8-14-21/h3-8,11-14,17,19H,9-10,15-16,18H2,1-2H3,(H,29,30)
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Chemical Name |
2-[4-[(5,6-diphenylpyrazin-2-yl)-propan-2-ylamino]butoxy]acetic acid
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Synonyms |
ACT 333679; MRE 269; MRE-269; ACT333679; ACT-333679; MRE269
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 50~84 mg/mL (119.2~200.2 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.96 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.96 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3837 mL | 11.9184 mL | 23.8368 mL | |
5 mM | 0.4767 mL | 2.3837 mL | 4.7674 mL | |
10 mM | 0.2384 mL | 1.1918 mL | 2.3837 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02206204 | Completed | Drug: selexipag Drug: moxifloxacin |
Safety Cardiodynamics Pharmacokinetics Tolerability |
Actelion | June 2012 | Phase 1 |