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Ex26 is a peripherally-restricted biphenylcarboxamide derivative that acts as a highly potent and subtype-selective S1P1 antagonist (IC50 = 0.93 nM against S1PR1 and >3.1 μM against S1PR2/3/4/5). Ex26 significantly elevates CpG-A-stimulated interferon (IFN) production in plasmacytoid dendritic cell culture (10 μM) and prevents S1P1 agonist-induced S1P1 receptor internalization and polyubiquitinylation in HEK cells (0.1-1,000 nM). Ex26 induces lymphocyte sequestration (ED50 = 0.06 mg/kg, i.p.) in lymph nodes and pulmonary edema (2 hr post 30 mg/kg i.p.) in mice, leading to the inhibition of lymphocyte and thymocyte egress (0.1 mg/kg/hr continuously for 3 days after a loading dose of 3 mg/kg). Ex26 has been shown to ameliorate experimental autoimmune encephalomyelitis (EAE) in a mouse MS model and elevate CpG-A-stimulated serum IFN upregulation in mice in vivo (30 mg/kg/d, i.p.).
| Molecular Weight | 494.98 |
| Formula | C28H28ClFN2O3 |
| CAS Number | 1233332-37-0 |
| Solubility (25°C) | DMSO: 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related S1P Receptor Products |
|---|
| FTY720 hydrochloride
Fingolimod (FTY720) HCl is a 1-phospho-neuraminol S1P receptor antagonist with an IC50 of 0.33 nM. , FTY720 can dephosphorylate AMPK by activating PP2A and reduce the expression level of phosphorylated eEF2K, ultimately leading to ADCD and iron death in human multiple myeloma cells. |
| BAF312
BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. |
| SEW2871
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. |
| CYM-5442
CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 can easily penetrate the central nervous system (CNS). |
| JTE 013
JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. |
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