Etrasimod (ADP334) | S1P1 antagonist | Probechem Biochemicals

Chemical Structure : Etrasimod

CAS No.: 1206123-37-6

Etrasimod (APD334, APD-334)

Catalog No.: PC-43209Not For Human Use, Lab Use Only.

Etrasimod (APD334) is a potent, selective, centrally available S1P1 receptor antagonist with β-arrestin EC50 of 6.1 nM, internalizes human S1P1 in CHO cells expressing HA tagged S1P1 with IC50 of 1.88 nM.

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10 mg	$188	In stock
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Biological Activity

Etrasimod (APD334) is a potent, selective, centrally available S1P1 receptor antagonist with β-arrestin EC50 of 6.1 nM, internalizes human S1P1 in CHO cells expressing HA tagged S1P1 with IC50 of 1.88 nM.
Etrasimod (APD334) produces robust lymphocyte lowering effect (IC50=0.1 uM in mice).
Etrasimod (APD334) shows effectivity in mouse experimental autoimmune encephalomyelitis (EAE) model of MS and a rat collagen induced arthritis (CIA) model, orally active.

Physicochemical Properties

M.Wt	457.4847
Formula	C26H26F3NO3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: ≥ 28 mg/mL
Chemical Name/SMILES	Cyclopent[b]indole-3-acetic acid, 7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydro-, (3R)-

References

1. Buzard DJ, et al. ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7.

2. Peyrin-Biroulet L, et al. Autoimmun Rev. 2017 May;16(5):495-503.

3. Nielsen OH, et al. Expert Opin Investig Drugs. 2016 Jun;25(6):709-18.

Etrasimod (APD334, APD-334)

Biological Activity

Physicochemical Properties

References

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