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FK-506-13C-d2

(Synonyms: 他克莫司-13C,FK506-13C,d2; Fujimycin-13C,d2; FR900506-13C,d2) 目录号 : GC47352

An internal standard for the quantification of FK-506

FK-506-13C-d2 Chemical Structure

Cas No.:1356841-89-8

规格 价格 库存 购买数量
500ug
¥7,340.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.1 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.2 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.3 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+.

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)

化学性质

Cas No. 1356841-89-8 SDF
别名 他克莫司-13C,FK506-13C,d2; Fujimycin-13C,d2; FR900506-13C,d2
Canonical SMILES O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H]3C/C=[13C]([2H])\[2H])=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@H](O)CC4)[C@H](C)[C@@H](O)CC3=O
分子式 C43[13C]H67D2NO12 分子量 807
溶解度 DMSO : 150 mg/mL (185.87 mM; Need ultrasonic and warming); Ethanol : ≥ 30 mg/mL (37.17 mM); DMF : ≥ 30 mg/mL (37.17 mM); DMSO : ≥ 20 mg/mL (24.78 mM) 储存条件 Store at -20°C,protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 1.2392 mL 6.1958 mL 12.3916 mL
5 mM 0.2478 mL 1.2392 mL 2.4783 mL
10 mM 0.1239 mL 0.6196 mL 1.2392 mL
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