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Tocris/Selexipag/3351/50/50 mg

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货号: 3351/50

品牌: Tocris

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Description: Selective prostacyclin IP₁ receptor agonist

Alternative Names: NS-304, ACT-293987

Chemical Name: 2-[4-[(5,6-Diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]-N-(methylsulfonyl)acetamide

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective prostacyclin IP₁ receptor agonist (K_i values are 260 and 2100 nM and for human and rat IP receptors, and >10 μM for EP_1-4, DP, FP, and TP receptors). Prodrug for the active form of MRE 26. Ameliorates vascular endothelial dysfunction and increases femoral skin blood flow in rats. Orally available.

Licensing Information

Sold with the permission of Nippon Shinyaku Co.

Compound Libraries

Selexipag is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	496.62
Formula	C₂₆H₃₂N₄O₄S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	475086-01-2
PubChem ID	9913767
InChI Key	QXWZQTURMXZVHJ-UHFFFAOYSA-N
Smiles	CC(C)N(CCCCOCC(NS(C)(=O)=O)=O)C1=NC(C3=CC=CC=C3)=C(C2=CC=CC=C2)N=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	49.66	100

Preparing Stock Solutions

The following data is based on the product molecular weight 496.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.01 mL	10.07 mL	20.14 mL
5 mM	0.4 mL	2.01 mL	4.03 mL
10 mM	0.2 mL	1.01 mL	2.01 mL
50 mM	0.04 mL	0.2 mL	0.4 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Kuwano et al (2007) 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. 322 1181 PMID: 17545310

Kuwano et al (2008) A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses of its active fo J.Pharmacol.Exp.Ther. 326 691 PMID: 18552131

Morrison et al (2010) Selexipag: a selective prostacyclin receptor agonist that does not affect rat gastric function. J.Pharmacol.Exp.Ther. 335 249 PMID: 20660124

Keywords: Selexipag, supplier, NS304, Selexipag, agonists, prostaglandin, PGI2, analogue, IP, receptors, hypertension, vascular, supplier, NS-304, ACT-293987, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience

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