>>Signaling Pathways>> GPCR/G protein>> S1P receptor inhibitor>>FTY720 Phosphate

FTY720 Phosphate (Synonyms: FTY720P)

Catalog No.GC13712

sphingosine-1-phosphate (S1P) receptors agonist

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FTY720 Phosphate Chemical Structure

Cas No.: 402615-91-2

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$455.00
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1mg
US$108.00
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5mg
US$414.00
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Sample solution is provided at 25 µL, 10mM.

Description of FTY720 Phosphate

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.

Chemical Properties of FTY720 Phosphate

Cas No. 402615-91-2 SDF
Synonyms FTY720P
Chemical Name 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
Formula C19H34NO5P M.Wt 387.5
Solubility ≤0.5mg/ml in chloroform Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of FTY720 Phosphate

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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