F-4900 FK-506, >99%

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.

ATH-123 ATH-122 ATH-121 ATH-120 ATH-119 ATH-118 ATH-117 ATH-116 ATH-115 ATH-114 ATH-113 ATH-112 ATH-111 ATH-110

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• More than 920 labs worldwide have purchased FK-506 from LC Labs (either directly from us or from our many distributors, many of whom resell under their own labels).
• Ascomycin level is less than 0.9%.
• 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).
• Water content of LC Labs' F-4900, FK506:
  PLEASE NOTE: We do not attempt or purport to control the water content of our FK-506 product.  We use the CAS number assigned to the anhydrous form.
  
  Here are the water levels of our most recent lots, as determined by elemental analysis:
  ATH-123   0.9 eq
  ATH-122   0.9 eq
  ATH-121   1.0 eq
  ATH-120   1.0 eq
  ATH-119   none
  ATH-118   0.8 eq
  ATH-117   0.8 eq
  ATH-116   0.8 eq
• Drying compounds to the point of complete absence of water is often a completely futile exercise, because many organic compounds rapidly rehydrate when opened to the air, even for short periods of time, in normal use.  The rate and avidity of such re-hydration is sometimes very impressive, indeed awesome in some cases, even for compounds that are not generally recognized as being hydroscopic.
• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
• Please see also our other standard immunosuppressant products:
  A-1040 Ascomycin
  C-6000 Cyclosporin A
  E-4040 Everolimus
  F-4633 Fingolimod Hydrochloride Salt
  R-5000 Rapamycin
  T-8040 Temsirolimus
  T-1377 Tofacitinib, Free Base
  T-1399 Tofacitinib,Citrate
  
  
  
• The CAS number for the anhydrous form of FK-506 is given above. The CAS number for FK-506 monohydrate is 109581-93-3.
• FK-506 (Tacrolimus) is the active ingredient in the drug sold under the trade names Fujimycin® and Prograf®. NOTE: THE FK-506 (TACROLIMUS) RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT FUJIMYCIN® NOR PROGRAF® AND IS NOT FOR HUMAN USE.