Home Categories Biochemical Engineering Tacrolimus
A7639712

Tacrolimus , ≥98%(HPLC) , 104987-11-3

Synonym(s):
FK-506 monohydrate;FK-506, Streptomyces sp. - CAS 104987-11-3 - Calbiochem;Tacrolimus

CAS NO.:104987-11-3

Empirical Formula: C44 H69 N O12

Molecular Weight: 804.02

MDL number: MFCD00869853

EINECS: 1308068-626-2

Pack Size Price Stock Quantity
50MG RMB102.40 In Stock
250mg RMB396.80 In Stock
1g RMB1030.40 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 113-115°C
Boiling point: 871.7±75.0 °C(Predicted)
Density  1.19±0.1 g/cm3(Predicted)
Flash point: 2℃
storage temp.  Sealed in dry,Store in freezer, under -20°C
solubility  DMSO: >3 mg/mL
form  solid
pka 9.97±0.70(Predicted)
color  white
optical activity +62.223 (CHCl3)
Water Solubility  Freely soluble in DMSO or ethanol. Poorly soluble in water.Soluble in dimethyl sulfoxide, ethanol, water, acetone, chloroform, ethyl acetate, ether, methanol and dimethyl formamide.
BCS Class 2
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
InChIKey QJJXYPPXXYFBGM-LFZNUXCKSA-N

Description and Uses

FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A and rapamycin . Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation. The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors. In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors leaky to Ca2+.

Tacrolimus (fujimycin) was discovered as a potent inhibitor of IL2 production in a targeted search for novel immunosuppressants. Tacrolimus acts by blocking T cell proliferation in vitro by inhibiting the generation of several lymphokines, notably the original target IL-2. Tacrolimus inhibits the activity of FK-506 binding protein, Ca2+-dependent phosphatase and calcineurin, and activates NF-κB through phosphorylation and degradation of IκBα.

Safety

Symbol(GHS) 
GHS06,GHS08
Signal word  Danger
Hazard statements  H301-H361f-H373
Precautionary statements  P202-P260-P264-P270-P280-P301+P310
Hazard Codes  T,Xi,Xn,F
Risk Statements  25-36/37/38-36-20/21/22-11
Safety Statements  45-36-26-36/37-16-60-20
RIDADR  UN 2811 6.1/PG 3
WGK Germany  3
RTECS  KD4201200
HazardClass  6.1
HS Code  29349990

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