General description

An orally bioavailable polar head group lacking carbamoylnicotinamide compound that acts as a potent and reversible agonist of hS1P₁ receptor (EC₅₀ = 35 nM with 96% efficacy) with substantial to excellent selectivity over hS1P₅ (EC₅₀ = 4.3 µM with 58% efficacy) and hS1P_2-4 (EC₅₀ >25 µM). Minimally affects the activities of hERG (IC₅₀ >10 µM) and cytochrome p450 isozymes (IC₅₀ >30 µM for 3A4 and 2D6), and exhibits desirable microsomal stability and aqueous solubility, Shown to efficiently reduce the circulating lymphocyte levels in rats (1 mg/kg, p.o.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Pennington, L.D., et al. 2011. Bioorg. Med. Chem. Lett.22, 527.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)