[CAS NO. 1230487-00-9]  Siponimod (BAF312)

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PRODUCTS SPECIFICATIONS [1230487-00-9]

Catalog
SLK-S7179
Brand
Selleck
CAS
1230487-00-9

DESCRIPTION [1230487-00-9]

Overview

MDLMFCD26142651
Molecular Weight516.6
Molecular FormulaC29H35F3N2O3
SMILESC(F)(F)(F)C1=C(C=CC(CO/N=C(\C)/C2=CC(CC)=C(CN3CC(C(O)=O)C3)C=C2)=C1)C4CCCCC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.9357 mL9.6787 mL19.3573 mL
5 mM0.3871 mL1.9357 mL3.8715 mL
10 mM0.1936 mL0.9679 mL1.9357 mL
50 mM0.0387 mL0.1936 mL0.3871 mL

Description

BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for and receptors with of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.

Targets

S1P1 receptor [1]S1P5 receptor [1]
0.39 nM(EC50)0.98 nM(EC50)

In vitro

BAF312 (Siponimod) is a potent and selective S1P receptor agonist, with EC50 of 0.39 nM and 0.98 nM for S1P and S1Preceptors, exhibits >1000-fold selectivity over S1P, S1P and S1P receptors. BAF312 (1 h at 1 μM) promotes prominent internalization of S1P1 receptors by 91%.

In vivo

BAF312 effectively suppresses encephalomyelitis (EAE) in rats by internalizing S1P receptors, rendering them insensitive to the egress signal from lymph nodes. BAF312 significantly reduces clinical scores when dosed prophylactically or therapeutically in mice at 0.3 mg/kg.