Fingolimod (hydrochloride)
Fingolimod is an immune modulator, a prodrug form of the sphingosine-1-phosphate (S1P) receptor agonist FTY720 phosphate (Item No. 10008639), and a derivative of myriocin (Item No. 63150).{11284} It selectively inhibits calcium-dependent cytosolic phospholipase A2 (cPLA2) over calcium-independent PLA2 (iPLA2) and secretory PLA2 (sPLA2) (Type V) when used at a concentration of 800 pmol and inhibits S1P lyase when used at concentrations ranging from 0.3 to 30 µM.{14604,65852} Fingolimod (1 mg/kg) decreases the number of circulating lymphocytes in mice.{65852} It increases skin allograft survival in rats when administered at doses ranging from 0.3 to 3 mg/kg.{16428} Fingolimod (0.3 mg/kg) prevents disease development in a rat model of experimental autoimmune encephalomyelitis (EAE) induced by immunization with an emulsion of bovine spinal cord in complete Freund’s adjuvant.{11284} Formulations containing fingolimod have been used in the treatment of multiple sclerosis.
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