Fingolimod (FTY-720)

製品コードS5950 バッチS595002

化学情報

	Synonyms	FTY-720A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₉H₃₃NO₂
	分子量	307.47	CAS No.	162359-55-9
Solubility (25°C)*	体外	Ethanol	11 mg/mL (35.77 mM)
		DMSO	10 mg/mL (32.52 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
in vitro	The main immunomodulatory mechanism of action of fingolimod is based on its effect on lymphocyte homing. It reversibly redistributes T and B cells from the circulation to secondary lymphoid organs like peripheral and mesenteric lymph nodes and Peyer's patches, thereby causing a state of peripheral lymphopenia^[1].
in vivo	SphK2 is the only enzyme which activates fingolimod in vivo,since only Sphk2 knockout mice are resistant to fingolimod-induced lymphopenia. A major advantage of fingolimod as a therapeutic agent is the possibility of its oral application. Absorption is food-independent and slow (maximal plasma concentration after 12-16 h), but extensive, and its bioavailability is high (93%). It reaches steady state concentrations after 1-2 months during daily intake. Fingolimod shows high plasma protein binding (>99.7%), mainly to albumin, and in contrast to S1P, there is no evidence for fingolimod binding to ApoM/HDL. It has a large volume of distribution of approx. 20L/kg and shows slow blood clearance (6.3±2.3 L/h), resulting in a half-life of 6-9 days^[1]. Fingolimod alleviates disease burden in immune-mediated animal models of multiple sclerosis^[2].

製品説明

Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.

in vitro

The main immunomodulatory mechanism of action of fingolimod is based on its effect on lymphocyte homing. It reversibly redistributes T and B cells from the circulation to secondary lymphoid organs like peripheral and mesenteric lymph nodes and Peyer's patches, thereby causing a state of peripheral lymphopenia^[1].

in vivo

SphK2 is the only enzyme which activates fingolimod in vivo,since only Sphk2 knockout mice are resistant to fingolimod-induced lymphopenia. A major advantage of fingolimod as a therapeutic agent is the possibility of its oral application. Absorption is food-independent and slow (maximal plasma concentration after 12-16 h), but extensive, and its bioavailability is high (93%). It reaches steady state concentrations after 1-2 months during daily intake. Fingolimod shows high plasma protein binding (>99.7%), mainly to albumin, and in contrast to S1P, there is no evidence for fingolimod binding to ApoM/HDL. It has a large volume of distribution of approx. 20L/kg and shows slow blood clearance (6.3±2.3 L/h), resulting in a half-life of 6-9 days^[1].

Fingolimod alleviates disease burden in immune-mediated animal models of multiple sclerosis^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NSCLC cells
	濃度	10 μM
	反応時間	72 h
	実験の流れ	Cells were treated with various concentrations of drug for 72 h.
動物実験	動物モデル	C57/B6 mice
	投薬量	1 mg/kg
	投与方法	o.g.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A novel isoxazole compound CM2-II-173 inhibits the invasive phenotype of triple-negative breast cancer cells [ Oncol Res, 2023, 31(6):867-875]	PubMed: 37744269
Selective delivery of low-affinity IL-2 to PD-1+ T cells rejuvenates antitumor immunity with reduced toxicity [ J Clin Invest, 2022, 132(3)e153604]	PubMed: 35104810
Selective delivery of low-affinity IL-2 to PD-1+ T cells rejuvenates antitumor immunity with reduced toxicity [ J Clin Invest, 2022, 132(3)e153604]	PubMed: 35104810
Intratumoral administration of STING-activating nanovaccine enhances T cell immunotherapy [ J Immunother Cancer, 2022, 10(5)e003960]	PubMed: 35623658
The central role of Sphingosine kinase 1 in the development of neuroendocrine prostate cancer (NEPC): A new targeted therapy of NEPC [ Clin Transl Med, 2022, 12(2):e695]	PubMed: 35184376
The sphingosine kinase inhibitor SKI-V suppresses cervical cancer cell growth [ Int J Biol Sci, 2022, 18(7):2994-3005]	PubMed: 35541904
Targeting sphingosine kinase 1/2 by a novel dual inhibitor SKI-349 suppresses non-small cell lung cancer cell growth [ Cell Death Dis, 2022, 13(7):602]	PubMed: 35831279
Efficacy of Vafidemstat in Experimental Autoimmune Encephalomyelitis Highlights the KDM1A/RCOR1/HDAC Epigenetic Axis in Multiple Sclerosis [ Pharmaceutics, 2022, 14(7)1420]	PubMed: 35890315
The immunostimulatory RNA RN7SL1 enables CAR-T cells to enhance autonomous and endogenous immune function [ Cell, 2021, 184(19):4981-4995.e14]	PubMed: 34464586
ChenThe interplay between fibroblast-like synovial and vascular endothelial cells leads to angiogenesis via the sphingosine-1-phosphate-induced RhoA-F-Actin and Ras-Erk1/2 pathways and the intervention of geniposide [ Phytother Res, 2021, 10.1002/ptr.7211]	PubMed: 34327764

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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