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Selexipag [475086-01-2]

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Referencia NB-64-20599-5mg

embalaje : 5mg

Marca : Neo Biotech

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Selexipag

(Synonyms: Uptravi, NS-304, ACT-293987) Copy Product Info

Synonyms: Uptravi, NS-304, ACT-293987

Catalog No. T3216 Copy Product Info

Purity: >99.99%

Selexipag (ACT-293987)(NS-304) is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH).

Cas No. 475086-01-2

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.98%

Appearance:Solid

Color:White

Product Information

Bioactivity

Description	Selexipag (ACT-293987)(NS-304) is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH).
Targets & IC50	IP (human):260 nM (Ki)
In vitro	Selexipag is an orally available and long-acting IP receptor agonist prodrug, and its active form, MRE-269, is highly selective for the IP receptor. Selexipag inhibits the binding of [3H]Iloprost to the human and rat IP receptors in a concentration-dependent manner. The Ki is 260 nM for the human IP receptor and 2100 nM for the rat IP receptor. The intracellular cAMP levels in hIP-CHO cells are increased in a concentration-dependent manner by treatment with Selexipag with EC50 of 177 nM. Selexipag also inhibits platelet aggregation in humans and monkeys with IC50 values of 5.5 and 3.4 μM, respectively, but it shows no inhibition in dogs (IC50 of >100 μM)[1].
In vivo	The Cmax of MRE-269 after oral administration of Selexipag is 1.1 μg/mL in rats and 9.0 μg/mL in dogs. Selexipag at 1 or 3 mg/kg increases FSBF in anesthetized rats for more than 4 h after intraduodenal administration in a dose-dependent manner. In particular, Selexipag at 3 mg/kg causes a sustained increase in FSBF and exhibits a maximal increase of 93% in FSBF 1 h after administration[1].
Synonyms	Uptravi, NS-304, ACT-293987
Cell Research	NS-304 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. CHO cells expressing the human IP receptor (hIP-CHO cells) are seeded at 1×105 cells/well in a 24-well plate and cultured for 48 h. The cells are washed with Dulbecco's phosphate-buffered saline without divalent cations, preincubated in the medium for 1 h at 37°C, and then incubated for 15 min at 37°C with medium containing each drug in the presence of 500 μM 3-isobutyl-1-methylxanthine. The medium is removed, and perchloric acid solution is added to terminate the reaction. Intracellular cAMP levels are measured by enzymelinked immunosorbent assay[1].

Chemical Properties

Molecular Weight	496.62
Formula	C₂₆H₃₂N₄O₄S
Cas No.	475086-01-2
Smiles	N(CCCCOCC(NS(C)(=O)=O)=O)(C(C)C)C=1N=C(C(=NC1)C2=CC=CC=C2)C3=CC=CC=C3
Relative Density.	1.210 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (503.4 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.03 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0136 mL	10.0681 mL	20.1361 mL	100.6806 mL
5 mM	0.4027 mL	2.0136 mL	4.0272 mL	20.1361 mL
10 mM	0.2014 mL	1.0068 mL	2.0136 mL	10.0681 mL
20 mM	0.1007 mL	0.5034 mL	1.0068 mL	5.0340 mL
50 mM	0.0403 mL	0.2014 mL	0.4027 mL	2.0136 mL
100 mM	0.0201 mL	0.1007 mL	0.2014 mL	1.0068 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

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