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Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. After oral administration of amiselimod or fingolimod at 1 mg/kg, the concentration of amiselimod-P in rat heart tissue was relatively lower than that of fingolimod-P, potentially contributing to the minimal cardiac effects of amiselimod. Amiselimod-P showed potent selectivity for S1P1 , high selectivity for S1P5 , minimal agonist activity for S1P4 , no distinct agonist activity for S1P2 or S1P3 , and approximately 5-fold weaker GIRK activation than fingolimod-P. Amiselimod 0·2 mg and 0·4 mg significantly reduced the total number of gadolinium-enhanced T1-weighted lesions.
| Molecular Weight | 413.9 |
| Formula | C19H31ClF3NO3 |
| CAS Number | 942398-84-7 |
| Solubility (25°C) | 30 mg/mL in DMSO |
| 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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