Free shipping on all orders over $ 500

BAF312

Cat. No. M2428
BAF312 Structure
Synonym:

Siponimod

Size Price Availability Quantity
5mg USD 81  USD90 In stock
10mg USD 121.5  USD135 In stock
50mg USD 405  USD450 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
Cell lines CHO cells
Preparation method Agonist-mediated internalization of S1P1 receptors in CHO cells analysed by flow cytometry
Myc-tag hS1P1 cells were incubated for 1 h with agonist at 37°C in standard culture medium followed by a PBS wash. An aliquot was kept on ice for 3 h, while another aliquot was left for 3 (or 12) h in culture medium (no agonist) at 37°C. The cells were then incubated either with 4 µg·mL−1 monoclonal mouse anti C-myc IgG1 (Roche Applied Science, Mannheim, Germany) antibody or with isotype control mouse IgG1 (Pharmingen, BD Biosciences, Basel, Switzerland) for 60 min at 4°C, followed by an incubation with 1 µg·mL−1 of Alexa488-labelled goat anti-mouse secondary conjugates (Molecular Probes, Juro Supply, Luzern, Switzerland). The cells were subjected to flow cytometry measurements using 10000 viable cells per sample.
Concentrations 1 μM
Incubation time 1h
Animal Experiment
Animal models EAE model in the DA rat
Formulation 1% aqueous carboxy-methylcellulose (C-4888, Sigma Chemical Co, St Louis, MO)
Dosages 0.03, 0.3 and 3 mg/kg once daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 516.6
Formula C29H35F3N2O3
CAS Number 1230487-00-9
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate.
Gergely P, et al. Br J Pharmacol. 2012 Nov;167(5):1035-47. PMID: 22646698.

Related S1P Receptor Products
Etrasimod (APD334)

Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor, with IC50 of 1.88 nM in CHO cells.

PF-543 Citrate

PF-543 Citrate is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM.

Opaganib (ABC294640)

Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM.

NIBR-0213

NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist.

A-971432

A-971432 is an orally bioavailable, non-clastogenic, azetidinecarboxylate compound that acts as a highly potent and selective sphingosine-1-phosphate receptor 5 agonist (IC50 = 6 nM/S1P5, 362 nM/S1P1 and >10 μM/S1P3 in a radio-ligand binding assay).

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BAF312, Siponimod supplier, S1P Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.