Tacrolimus (FK506) 104987-11-3

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Molecular Weight: 804.02 FK-506 is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex.


FK-506 and cyclosporin A block translocation of the cytoplasmic
component without affecting synthesis of the nuclear subunit in T
lymphocytes. FK-506 prevents T-cell proliferation by
inhibiting a Ca(2+)-dependent event required for induction of
interleukin-2 transcription. FK 506 binds to distinct
families of intracellular Proteins (immunophilins) termed cyclophilins
and FK 506-binding proteins (FKBPs).


FK-506 specifically inhibits
cellular calcineurin at drug concentrations that inhibit interleukin 2
production in activated T cells. FK-506 and CsA exert
nearly identical biological effects in cells by inhibiting the same
subset of early calcium-associated events involved in lymphokine
expression, Apoptosis, and degranulation. FK-506 binds to a family of
intracellular receptors termed the FK-506 binding proteins (FKBPs)


FK-506 results in increase in the paw and tail withdrawal threshold as
revealed by behavioral pain assessment in rats against hyperalgesic and
allodynic stimuli. FK-506 also leads to a decrease in the serum nitrate
and thiobarbituric acid reactive substance (TBARS) levels along with
reduction in tissue myeloperoxidase (MPO) and total calcium levels,
whereas, rise in tissue reduced glutathione levels in rats. FK-506
ameliorates the increase in the neuronal edema and axonal degeneration
in rats with ischemia reperfusion (I/R).


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	804.02
Formula	C44H69NO12
CAS No.	104987-11-3

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	FR900506

Solubility (25°C) *	In vitro	DMSO	94 mg/mL (116.91 mM)
		Water	<1 mg/mL (
		Ethanol	83 mg/mL (103.23 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	(3S,4R,5S,8R,9E...5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone

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