|Chemical Name:||(E)-1-(4-(1-(((4-cyclohexyl-3-(trifluoromethyl)benzyl)oxy)imino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid|
|Solubility:||DMSO up to 100 mM|
|Storage:||Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year|
BAF312 is a next-generation potent sphingosine 1-phosphate (S1P) receptor agonist, selective for S1P1 (EC50 ~0.39 nM) and S1P5 (EC50 ~0.98 nM). As S1P1 plays a central role in lymphocyte egress from lymph nodes and is a validated drug target in immune-mediated diseases, BAF312 is currently in clinical trials to treat multiple sclerosis.
How to Use:
In vitro: BAF312 was used at 0.1µM in vitro.
In vivo: BAF312 was orally dosed once daily at 0.3-3 mg/kg in chronic EAE, DA rats and was shown good efficacy.
- Gergely P, et al. The selective S1P receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate: translation from preclinical to clinical studies. (2012) Br J Pharmacol. 167(5):1035-47.
- Pan SF, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. (2013) ACS Med. Chem. Lett. In press.
- Fryer RM, et al. The clinically-tested S1P receptor agonists, FTY720 and BAF312, demonstrate subtype-specific bradycardia (S1P₁) and hypertension (S1P₃) in rat. (2012) PLoS One. (12):e52985.
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