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BAF312 (Siponimod)

Catalog No.
B3225
S1P agonist,potent and selective
Grouped product items
SizePriceStock Qty
5mg
$80.00
In stock
25mg
$230.00
In stock
100mg
$580.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

BAF312 is a potent and selective agonist of S1P with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively [1].

BAF312 has shown >1000-fold selectivity for S1P1 versus S1P2, S1P3 and S1P4 receptors [1]. In vitro metabolism studies with liver microsomes have shown that the metabolic clearance of BAF312 is high in rat, low to moderate in monkey and human being, and low in dog and mouse. Moreover, BAF312 has been revealed to?dose-dependently reduce peripheral lymphocyte counts in Lewis rats [2].

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References:
[1] Gergely P1, Nuesslein-Hildesheim B, Guerini D, Brinkmann V, Traebert M, Bruns C, Pan S, Gray NS, Hinterding K, Cooke NG, Groenewegen A, Vitaliti A, Sing T, Luttringer O, Yang J, Gardin A, Wang N, Crumb WJ Jr, Saltzman M, Rosenberg M, Wallstr?m E. The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012 Nov;167(5):1035-47.
[2] Pan S1, Gray NS1, Gao W1, Mi Y1, Fan Y1, Wang X1, Tuntland T1, Che J1, Lefebvre S1, Chen Y1, Chu A1, Hinterding K2, Gardin A2, End P2, Heining P2, Bruns C2, Cooke NG2, Nuesslein-Hildesheim B2 .Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Jan 4;4(3):333-7.

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Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt516.6
Cas No.1230487-00-9
FormulaC29H35F3N2O3
Solubility≥194.8 mg/mL in DMSO; insoluble in H2O; ≥3.27 mg/mL in EtOH
Chemical Name1-[[4-[(E)-N-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-C-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid
SDFDownload SDF
Canonical SMILESCCC1=C(C=CC(=C1)C(=NOCC2=CC(=C(C=C2)C3CCCCC3)C(F)(F)F)C)CN4CC(C4)C(=O)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

human atrial myocytes

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.001-1000 nM

Applications

In human atrial myocytes, BAF312 concentration-dependently increased GIRK current amplitude with EC50 value of 15.8 nM and reached approximately 80% of the carbachol-induced maximal current activation.
Animal experiment [1, 2]:

Animal models

rat experimental autoimmune encephalomyelitis (EAE) model; Lewis rats

Dosage form

0.03, 0.3 or 3 mg/kg, orally administrated, 24 day; 1 mg/kg, orally administrated

Application

In rat experimental autoimmune encephalomyelitis (EAE) model, BAF312 starting on day 11 significantly inhibited established neurological deficits. BAF312 at 0.3 or 3 mg/kg caused a significant reduction of disease scores (AUC (area under the concentration–time curve) from days 12 to 34). In Lewis rats, BAF312 (Siponimod) (1 mg/kg) dose-dependently reduced peripheral lymphocyte counts. At the Tmax of 8 h postadministration, the lymphocyte counts were decreased by 88%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Gergely P1, Nuesslein-Hildesheim B, Guerini D, Brinkmann V, Traebert M, Bruns C, Pan S, Gray NS, Hinterding K, Cooke NG, Groenewegen A, Vitaliti A, Sing T, Luttringer O, Yang J, Gardin A, Wang N, Crumb WJ Jr, Saltzman M, Rosenberg M, Wallstrm E. The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012 Nov;167(5):1035-47.

[2] Pan S1, Gray NS1, Gao W1, Mi Y1, Fan Y1, Wang X1, Tuntland T1, Che J1, Lefebvre S1, Chen Y1, Chu A1, Hinterding K2, Gardin A2, End P2, Heining P2, Bruns C2, Cooke NG2, Nuesslein-Hildesheim B2 .Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Jan 4;4(3):333-7.

Biological Activity

Description BAF312 is a potent and selective agonist of S1P with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively
Targets S1P1 receptors S1P5 receptors        
IC50 0.39nM (EC50) 0.98nM (EC50)        

Quality Control