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Etrasimod

Catalog No. TQ0227   CAS 1206123-37-6
Synonyms: APD334

Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).

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Etrasimod Chemical Structure
Etrasimod, CAS 1206123-37-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 68.00
5 mg In stock $ 116.00
10 mg In stock $ 191.00
25 mg In stock $ 369.00
50 mg In stock $ 555.00
100 mg In stock $ 698.00
200 mg In stock $ 994.00
1 mL * 10 mM (in DMSO) In stock $ 116.00
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Purity: 99.77%
Purity: 99.17%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).
Targets&IC50 S1P1:1.88 nM (CHO cells)
In vitro In CHO cells expressing HA-tagged S1P1, APD334 is found to have an IC50 value of 1.88 nM. Moderate agonism at human S1P4 and S1P5 is observed but is reduced relative to S1P1, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P2 and S1P3.
In vivo APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high Cmax across all species. In both dog and monkey, a significant decrease in the volume of distribution (Vss) is observed relative to the rodent. Oral bioavailability is in the range of 40–100% and the terminal phase half-life varied from 6 h in monkey, to as long as 29 h in the dog.
Animal Research APD334 induced effects on blood lymphopenia are determined in male Sprague-Dawley rats. Briefly, male rats are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Rat blood samples are collected at 0, 1, 3, 5, 8, 16, 24, 32, 48 and 72 hours post-dose. APD334 induced effects on blood lymphopenia are determined in male BALB/c mice. Briefly, male mice are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Mouse blood samples are taken at 0, 1, 3, 5, 8, 16, 24 and 32 hours post-dose.
Synonyms APD334
Molecular Weight 457.48
Formula C26H26F3NO3
CAS No. 1206123-37-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (54.64 mM)

TargetMolReferences and Literature

1. Buzard DJ, et al. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor. ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Bioactive Compounds Library Max Pediatric Drug Library GPCR Compound Library Human Metabolite Library Bioactive Compound Library Inhibitor Library NO PAINS Compound Library Approved Drug Library

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CYM-5541 LX-2931 Vibozilimod Sphingosine-1-phosphate Peretinoin ASP-4058 Phorbol 12-myristate 13-acetate MP-A08

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Keywords

Etrasimod 1206123-37-6 GPCR/G Protein S1P Receptor LPL Receptor Inhibitor inhibit APD-334 APD334 Lysophospholipid Receptor APD 334 inhibitor

 

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