Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Selexipag (NS-304; NS304; ACT-293987; ACT293987; Uptravi) is a novel and potent prodrug of ACT-333679 (MRE-269) acting as non-prostanoid IP receptor agonist and has been approved as a medication for the treatment of pulmonary arterial hypertension. Selexipag and its active metabolite, ACT-333679 (MRE-269), are agonists of the prostacyclin receptor, which can cause vasodilation in the pulmonary circulation.
ln Vitro |
The long-acting oral prodrug selexipag (NS-304) is an IP receptor agonist whose active form, MRE-269, is very selective for IP receptors. [3H]Iloprost binding to human and rat IP receptors is inhibited by selexipag (NS-304) in a concentration-dependent manner. The rat IP receptor has a Ki of 2100 nM and the human IP receptor has a Ki of 260 nM. With an EC50 of 177nM, intracellular cAMP levels in hIP-CHO cells rose in a concentration-dependent manner upon treatment with selenium (NS-304). With IC50 values of 5.5 and 3.4 μM, respectively, selexipag (NS-304) similarly prevents platelet aggregation in humans and monkeys, but not in dogs (IC50 > 100 μM) [1].
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ln Vivo |
After NS-304 was given orally to rats, the Cmax of MRE-269 was 1.1 μg/mL and in dogs, it was 9.0 μg/mL. In anesthetized rats, selexipag (NS-304) administered intradually at doses of 1 or 3 mg/kg enhances FSBF during a 4-hour period. Specifically, Selelexipag (NS-304) at 3 mg/kg increased FSBF over time, reaching a maximal rise of 93% in FSBF within an hour of dosing [1].
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References |
[1]. Kuwano K, et al. 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. J Pharmacol Exp Ther. 2007 Sep;322(3):1181-8.
[2]. Mous DS, et al. Treatment of rat congenital diaphragmatic hernia with sildenafil and NS-304, selexipag's active compound, at the pseudoglandular stage improves lung vasculature. Am J Physiol Lung Cell Mol Physiol. 2018 May 10 |
Molecular Formula |
C26H32N4O4S
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Molecular Weight |
496.62
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Exact Mass |
496.21443
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CAS # |
475086-01-2
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Related CAS # |
Selexipag-d7;1265295-21-3;Selexipag-d6;1265295-92-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S(C([H])([H])[H])(N([H])C(C([H])([H])OC([H])([H])C([H])([H])C([H])([H])C([H])([H])N(C1=C([H])N=C(C2C([H])=C([H])C([H])=C([H])C=2[H])C(C2C([H])=C([H])C([H])=C([H])C=2[H])=N1)C([H])(C([H])([H])[H])C([H])([H])[H])=O)(=O)=O
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Synonyms |
NS 304ACT293987NS-304 ACT 293987NS304 Uptravi ACT-293987 Selexipag
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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 mg/mL (~100.68 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (5.03 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 (5.03 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 | 2.0136 mL | 10.0681 mL | 20.1361 mL | |
5 mM | 0.4027 mL | 2.0136 mL | 4.0272 mL | |
10 mM | 0.2014 mL | 1.0068 mL | 2.0136 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.