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F-4900 FK-506, >99%

[Fujimycin] [Prograf] [Tacrolimus] [FK506] [FK 506]

M.W. 804.02

C44H69NO12

[104987-11-3]

M.I. 13:  9117

M.I. 14:  9025

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; maximum solubility in plain water is estimated to be about 10 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Ascomycin level is less than 0.5%.

• FK-506 is a potent immunosuppressant and in vitro T cell proliferation blocker.  It has been shown to disrupt calcineurin (also known as CaN or phosphatase 2B)-mediated signal transduction in T lymphocytes.  The compound interacts with its FK506-binding protein-12 (FKBP12).  The resulting complex, in turn, interferes with calcineurin substrate interaction.  Dumont, F.J.  "FK506, an immunosuppressant targeting calcineurin function."  Curr. Med. Chem. 7:  731-748 (2000).

• FK-506 inhibits FKBP activity resulting in an increase in the release of sarcoplasmic reticulum-derived calcium.  FK-506 also appears to inhibit Na(+)-Ca2+ exchange.  Unlike rapamycin, which also binds to FK506-binding protein-12, FKBP12 with or without bound FK506 has no effect on rat brain PKC activity in vitro.  McCall, E., et al.  "Effects of FK-506 on contraction and Ca2+ transients in rat cardiac myocytes."  Circ. Res. 79:  1110-1121 (1996).  Rokaw, M.D., et al.  "Rapamycin inhibits protein kinase C activity and stimulates Na+ transport in A6 cells."  J. Biol. Chem. 271:  32468-32473 (1996).

• 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-4633   Fingolimod, Hydrochloride Salt

  P-6040   Pimecrolimus

  R-5000   Rapamycin

  T-8040   Temsirolimus

  T-1377   Tofacitinib, Free Base

  Z-9040   Zotarolimus