Fingolimod, Hydrochloride Salt **

产品名称：Fingolimod, Hydrochloride Salt
产品货号：LC  F-4633  
产品规格：100 MG
Fingolimod (FTY720), a sphingosine 1-phosphate (S1P) analog, is a novel immunosuppressant drug that induces lymphopenia by preventing emergence of lymphocytes from lymph nodes.  Fingolimod is a sphingosine-1-phosphate receptor 1 modulator and is in phase III clinical trials for relapsing-remitting multiple sclerosis.  Chiba, K., et al. "Role of sphingosine 1-phosphate receptor type 1 in lymphocyte egress from secondary lymphoid tissues and thymus."  Cell Mol. Immunol. 3:  11-19 (2006).  Dev, K.K., et al.  "Brain sphingosine-1-phosphate receptors: implication for FTY720 in the treatment of multiple sclerosis."  Pharmacol. Ther. 117:  77-93 (2008).
Suppresses allotransplant rejections and autoimmune disorders in different animal models.  Kunzendorf, U., et al.  "FTY720—the first compound of a new promising class of immunosuppressive drugs."  Nephrol. Dial. Transplant. 19:  1677-1681 (2004).
Fingolimod appears to promote the survival of human and animal allografts by sequestering T lymphocytes within peripheral lymphoid tissue. Evidence for this mechanism of sequestration includes: (1) fingolimod drives T lymphocytes into peripheral lymph nodes in a chemokine dependent manner; (2) fingolimod downregulates sphingosine 1-phosphate receptors (S1PRs) on the T lymphocyte surface, preventing it from migrating along a S1P gradient; and (3) fingolimod blocks stromal gates on the abluminal side of the lymphatic endothelium.  Yopp, A.C., et al.  "Sphingosine 1-phosphate receptor modulators: a new class of immunosuppressants."  Clin. Transplant. 20:  788-795 (2006).
Fingolimod, as the hydrochloride salt, is the active ingredient in the drug sold under the trade names Gilenya® and Gilenia® by Novartis AG.  This drug is currently approved in at least one country for use in patients with relapsing forms of multiple sclerosis.  NOTE:  THE FINGOLIMOD, HYDROCHLORIDE SALT RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT GILENYA® nor GILENIA® AND IS NOT FOR HUMAN USE.  Gilenya® is a registered trademark of Novartis AG.  LC Laboratories is not affiliated with Novartis AG, and the fingolimod hydrochloride research compound sold by LC Laboratories is not manufactured by Novartis AG.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 100 mg/mL; soluble in ethanol at 100 mg/mL; very poorly soluble in water.  Up to 25 µL of a solution of 13.8 mg/mL (40 mM) fingolimod-HCl in 100% DMSO can be diluted into 5 mL of plain water without precipitation, giving a final concentration of 200 µM.  In contrast, even a 1-to-1,000 dilution of the same 13.8 mg/mL DMSO stock solution into a 10 mM phosphate-buffered saline at pH 7 results in a precipitate.  Thus, fingolimod-HCl solubility in PBS is likely to be well below 100 µM, perhaps as low as 1-10 µg/mL.  Either DMSO, ethanol or plain water should be used as the solvent until the final dilution is made into culture medium.  Buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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