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.

Reference:

1. 1. 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.
2. 2. Pan SF, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. (2013) ACS Med. Chem. Lett. In press.
3. 3. 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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