Tacrolimus-13C,d2 , ≥98% , 1356841-89-8

CAS NO.：1356841-89-8

Empirical Formula: C44H67D2NO12

Molecular Weight: 807.039

MDL number:

PRODUCT Properties

• storage temp.: -70°C
• solubility: Chloroform: Slightly Soluble,Methanol: Slightly Soluble
• form: A solid
• color: White to yellow

Description and Uses

FK-506-¹³C-d₂ contains two deuterium atoms located on the carbon-13 bond. It is intended for use as an internal standard for the quantification of FK-506 by GC- or LC-MS. FK-506 is a potent, clinically-useful immunosuppressant in the same molecular class as cyclosporin A and rapamycin. Its mechanism of action involves the formation of a high affinity complex (K_i = 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⁺.

A labelled immunosuppressant that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 binding protein, thereby reversing its effects on sarcoplasmic reticulum Ca+2 release. A representative lot contained a distribution of 20% d-1, 40% d-2 and 20% d-3.

Safety

• Symbol(GHS): GHS06
• Signal word: Danger
• Hazard statements: H301
• Precautionary statements: P264-P270-P301+P310-P321-P330-P405-P501
• RIDADR: UN 1648 3 / PGII