Etrasimod arginine is the L-arginine salt form of the selective S1P receptor modulator etrasimod (APD334), designed to enhance the solubility and formulation characteristics of the active pharmaceutical ingredient . Structurally, the salt consists of the (3R)-7-((4-cyclopentyl-3-(trifluoromethyl)phenyl)methoxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-ylacetate anion paired with a protonated L-arginine cation in a 1:1 stoichiometric ratio .
Etrasimod arginine is the pharmaceutically preferred salt form of the selective S1P receptor modulator etrasimod, designed to optimize the solubility and biopharmaceutical properties of this important immunomodulatory agent . As the clinically approved salt form under the brand name Velsipity, Etrasimod arginine provides the same potent and selective functional antagonism of S1P₁, S1P₄, and S1P₅ receptors as the free base, while offering enhanced aqueous solubility that facilitates oral formulation development . The L-arginine salt form of Etrasimod was selected to improve the drug's physicochemical properties without compromising its pharmacological activity or selectivity profile . This salt form is supplied as a solid with defined storage conditions—powder stable for up to 3 years at –20°C and 2 years at 4°C—making Etrasimod arginine an invaluable reference standard for both research and quality control applications . The compound's favorable solubility in DMSO and other organic solvents further supports its utility in a wide range of in vitro and in vivo studies .
Product Parameters
Parameter
Specification
Product Name
Etrasimod arginine
CAS Number
1206123-97-8
Molecular Formula
C₃₂H₄₀F₃N₅O₅
Molecular Weight
631.69 g/m
Appearance
White to beige powder
Solution
DMSO:2mg/ml , clear
Product Advantages
Clinically Approved Salt Form
Etrasimod arginine is the clinically approved salt form of etrasimod, marketed under the brand name Velsipity for the treatment of adult patients with moderately to severely active ulcerative colitis . This salt form was specifically selected for its favorable physicochemical and biopharmaceutical properties.
Enhanced Solubility and Formulation Properties
The L-arginine salt of Etrasimod was designed to improve the aqueous solubility and formulation characteristics of the active pharmaceutical ingredient . This enhanced solubility supports the development of oral formulations with improved bioavailability and dose consistency.
Defined Stability Profile for Research and Development
Etrasimod arginine offers a well-characterized stability profile: powder is stable for 3 years at –20°C and 2 years at 4°C, with solution stability of 6 months at –80°C and 1 month at –20°C . This defined stability supports long-term research programs and method validation studies.
Same Potent Pharmacology as the Free Base
The arginine salt form retains the full pharmacological activity of the free base—potent and selective functional antagonism of S1P₁, S1P₄, and S1P₅ receptors—without compromising its activity or selectivity profile .
Versatile Reference Standard Applications
Etrasimod arginine serves as both a reference standard for analytical method development and a research tool for salt form characterization. Its application spectrum includes QC testing, method validation, formulation development, and stability studies .
FAQ
Q1: What is the difference between Etrasimod and Etrasimod arginine?
A: Etrasimod (CAS 1206123-37-6) is the free base form of the compound, while Etrasimod arginine (CAS 1206123-97-8) is the L-arginine salt form in a 1:1 stoichiometric ratio . The arginine salt was developed to enhance the aqueous solubility and formulation properties of the active pharmaceutical ingredient, and it is the clinically approved form marketed under the brand name Velsipity.
Q2: What is the solubility of Etrasimod arginine?
A: Etrasimod arginine is soluble in DMSO . It may also dissolve in other organic solvents; researchers are advised to perform solubility tests in their specific assay media.
Storage Conditions
Store Etrasimod arginine powder in a tightly sealed container at –20°C for long-term storage (up to 3 years) or at 4°C for up to 2 years . For solutions, aliquot and store at –80°C for up to 6 months or at –20°C for up to 1 month . Protect from light and moisture, and store in a clean, dry, well-ventilated area away from strong oxidizing agents.
Shelf life: 3 years when stored as powder at –20°C; 2 years when stored as powder at 4°C; 6 months when stored in solution at –80°C; 1 month when stored in solution at –20°C .
Handling precautions: Use only in a fume hood. Wear chemical-resistant gloves, safety goggles, and a lab coat. Avoid generating dust or aerosols. Do not eat, drink or smoke in work areas. After handling, wash hands thoroughly. Refer to the Safety Data Sheet (SDS) for complete safety information.
Contact Us
When your pharmaceutical development program demands salt form integrity and uncompromising quality, Cosperpharm delivers. We invite you to connect with us to discuss how we can support your work with Etrasimod arginine—the clinically validated salt of this important S1P receptor modulator.
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