Etrasimod

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Etrasimod

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Cat No: 21661

Biochemicals - Receptor Pharmacology

Etrasimod is an orally bioavailable and potent antagonist of sphingosine-1-phosphate (S1P) receptors with EC50 values of 0.093, 0.44, 0.32, 0.34, and 0.32 nM for human, mouse, rat, dog, and monkey S1P1 receptors.{41302} It is selective for S1P1, S1P4,...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(3R)-7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydro-cyclopent[b]indole-3-acetic acid

Correlated keywords:

APD-334

Product Overview:
Etrasimod is an orally bioavailable and potent antagonist of sphingosine-1-phosphate (S1P) receptors with EC50 values of 0.093, 0.44, 0.32, 0.34, and 0.32 nM for human, mouse, rat, dog, and monkey S1P1 receptors.{41302} It is selective for S1P1, S1P4, and S1P5 receptors with EC50 values of 6.1, >10,000, >10,000, 147, and 24.4 nM for S1P1-5, respectively, in a β-arrestin assay. Etrasimod (1 mg/kg, i.v.) decreases peripheral lymphocytes in mouse, rat, dog, and monkey (IC50s = 101, 51, 58, and 98 nM, respectively). It delays or prevents the onset and severity of murine experimental autoimmune encephalomyelitis (EAE) when administered at 0.3, 1, or 3 mg/kg. It also leads to lower EAE disease scores relative to vehicle when administered after disease onset and is efficacious in a rat model of collagen-induced arthritis.

Size	1 mg
Shipping	dry ice
CAS Number	1206123-37-6
Molecular Formula	C₂₆H₂₆F₃NO₃
SMILES	OC(C[C@H]1CCC2=C1NC3=CC=C(OCC4=CC=C(C5CCCC5)C(C(F)(F)F)=C4)C=C32)=O
Molecular Weight	457,5
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2902.90
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.