An internal standard for the quantification of FK-506
货号:ajcx22496
CAS:1356841-89-8
分子式:C43[13C]H67D2NO12
分子量：807
溶解度:Chloroform: Slightly Soluble,Methanol: Slightly Soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

FK-506-¹³C-d₂contains 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.¹Its 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.²The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca²⁺releaseviathe ryanodine and inositol-(1,4,5)-trisphosphate (IP₃) receptors.³In the latter case, FKBP12 forms a tight complex with both ryanodine and IP₃receptors which can be disrupted by FK-506, thereby rendering the receptors "leaky" to Ca²⁺.

1.Schreiber, S.L.Chemistry and biology of the immunophilins and their immunosuppressive ligandsScience251(4991)283-287(1991) 2.Dumont, F.J.FK506, An immunosuppressant targeting calcineurin functionCurr. Med. Chem.7(7)731-748(2000) 3.Snyder, S.H., Sabatini, D.M., Lai, M.M., et al.Neural actions of immunophilin ligandsTrends Pharmacol. Sci.19(1)21-26(1998)