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F-4633 Fingolimod, Hydrochloride Salt, >99%

[FTY-720A] [FTY720]

M.W. 343.93

C19H33NO2•HCl

[162359-56-0]

M.I. 14:  4083

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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• 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).

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.

• Please see also our other standard immunosuppressant products:

  A-1040   Ascomycin

  C-6000   Cyclosporin A

  E-4040   Everolimus

  F-4900   FK-506

  P-6040   Pimecrolimus

  R-5000   Rapamycin

  T-8040   Temsirolimus

  T-1377   Tofacitinib, Free Base

  Z-9040   Zotarolimus