FTY720 Phosphate
(Synonyms: 2-氨基-2-(羟基甲基)-4-(4-辛基苯基)丁基磷酸二氢酯,FTY720P) 目录号 : GC13712The active metabolite of FTY720
Cas No.:402615-91-2
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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FTY720 is sphingosine-1-phosphate (S1P) receptors agonist [1]. FTY720 is a novel immunomodulatory agent derived from ISP-1 (myriocin), a fungal metabolite that exists in traditional Chinese herbal medicine. In higher eukaryotes, S1P is the ligand for five G-protein-coupled receptors. These S1P receptors are differentially expressed and regulate vascular maturation, angiogenesis, cardiac development and immunity. S1P receptors are important for directed cell movement [2].
In vitro: The phosphorylated FTY720 acted as agonist for a family of G protein-coupled receptors in vitro. FTY720 inhibited sphingosine-1-phosphate lyase activity [3]. FTY720 phosphate acted as a potent agonist at sphingosine-1-phosphate (S1P) receptors S1P1, S1P3, S1P4, and S1P5 with IC50 values of 0.2-6 nM [3].
In vivo: In a variety of transplant and autoimmune models, FTY720 was efficacious without inducing a generalized immunosuppressed state. FTY720 was effective in human kidney transplantation. FTY720 elicited lymphopenia resulting from a reversible redistribution of lymphocytes from circulation to secondary lymphoid tissues by unknown mechanisms. In a rodent model of multiple sclerosis, the phosphorylated FTY720 compound was a potent agonist at four s S1P receptors. Phosphorylation of FTY720 acted through sphingosine 1-phosphate signaling pathways to modulate chemotactic responses and lymphocyte trafficking [1]. FTY720 was phosphorylated in vivo. In mice, treatment with FTY720 inhibited tissue sphingosine-1-phosphate lyase activity, whereas lyase gene and protein expression were not significantly affected [3].
References:
[1] Brinkmann V, Davis M D, Heise C E, et al. The immune modulator FTY720 targets sphingosine 1-phosphate receptors[J]. Journal of Biological Chemistry, 2002, 277(24): 21453-21457.
[2] Spiegel S, Milstien S. Sphingosine-1-phosphate: an enigmatic signalling lipid[J]. Nature reviews Molecular cell biology, 2003, 4(5): 397-407.
[3] Bandhuvula P, Tam Y Y, Oskouian B, et al. The immune modulator FTY720 inhibits sphingosine-1-phosphate lyase activity[J]. Journal of Biological Chemistry, 2005, 280(40): 33697-33700.
Cas No. | 402615-91-2 | SDF | |
别名 | 2-氨基-2-(羟基甲基)-4-(4-辛基苯基)丁基磷酸二氢酯,FTY720P | ||
化学名 | 2-amino-2[2-(4-octylphenyl)ethyl]-1,3-propanediol, mono dihydrogen phosphate ester | ||
Canonical SMILES | CCCCCCCCC1=CC=C(CCC([NH3+])(COP([O-])(O)=O)CO)C=C1 | ||
分子式 | C19H34NO5P | 分子量 | 387.5 |
溶解度 | ≤0.5mg/ml in chloroform | 储存条件 | Store at -20°C |
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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5806 mL | 12.9032 mL | 25.8065 mL |
5 mM | 0.5161 mL | 2.5806 mL | 5.1613 mL |
10 mM | 0.2581 mL | 1.2903 mL | 2.5806 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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