Fingolimod hydrochloride | FTY720;Fingolimod (hydrochloride);Fingolimod HCl | 芬戈莫德盐酸盐 | LPL Receptor

Fingolimod HCl/盐酸芬戈莫德 {[allProObj[0].p_purity_real_show]}

货号：A151280 同义名： 芬戈莫德盐酸盐 / FTY720; Fingolimod (hydrochloride)

Fingolimod hydrochloride (FTY720) 是一种鞘氨醇的类似物，是一种有效的鞘氨醇 1-磷酸 (S1P) 受体调节剂。它被鞘氨醇激酶，特别是 SK2 磷酸化，并结合 S1PR1、3、4 和 5，诱导 S1P1 内化并抑制 S1P 活性。芬戈莫德盐酸盐还激活 pak1。

Fingolimod HCl/盐酸芬戈莫德化学结构
CAS号：162359-56-0

Fingolimod HCl/盐酸芬戈莫德 3D分子结构
CAS号：162359-56-0

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Fingolimod HCl/盐酸芬戈莫德生物活性

描述

Fingolimod HCl is the hydrochloride form of Fingolimod. Fingolimod is an S1p receptor modulator and also immunosuppressant. It can be primarily phosphorylated by SPHK2 to its active form fingolimod-P. Although fingolimod-P (but not parent fingolimod) could function as an agonist at S1P1, S1P4 and S1P5 receptors with EC50 values ranging in ~0.3–0.6nM and at 10- fold higher concentrations at S1P3 receptors with EC50 values of ~3 nM^[1], it caused S1P receptors to internalize from cell membranes and induce ubiquitinylation and proteasomal degradation of the receptor. That is, effects of Fingolimod are inhibitory in the longer term on S1P receptor function^[2]. Fingolimod was used to treat for multiple sclerosis. Culture with FTY720 at concentration of 1μM for 22 hours could stimulate survival of the oligodendrocyte progenitors, and an activation of both MEK/ERK1/2 and PI3K/Akt pathways dependent on transforming to fingolimod-P by SphK could be observed^[3]. Fingolimod is highly effective in experimental autoimmune encephalomyelitis model. Administration of fingolimod at dose of 0.03 to 1 mg/kg could significant improve the symptoms of chronic experimental autoimmune encephalomyelitis induced by myelin oligodendrocyte glycoprotein in mice due to the reduction of infiltration of myelin antigen-specific Th17 and Th1 cells into the central nervous system^[4].

作用机制

The aminodiol polar head group of fingolimod could be phosphorylated by SPHK2 and the lipophilic tail is important for interacting with the hydrophobic binding pocket of the S1P receptors^[1]

Fingolimod HCl/盐酸芬戈莫德细胞实验

Cell Line Panc05.04 cells BxPC3 and AsPC1 cells SMMC-7721 A549	Concentration	Treated Time	Description	References
Panc05.04 cells	5 µM	24 h	FTY-720 significantly inhibited the colony formation ability of SF3B1 K700E mutant Panc05.04 cells and reduced glucose uptake and lactate release.	Mol Oncol. 2021 Nov;15(11):3076-3090.
BxPC3 and AsPC1 cells	5 µM	24 h	FTY-720 did not significantly affect the glycolytic ability of BxPC3 and AsPC1 cells, but ectopic expression of SF3B1 K700E significantly promoted glucose uptake and lactate production.	Mol Oncol. 2021 Nov;15(11):3076-3090.
SMMC-7721	7.5 μM	24 h	To evaluate the autophagy induced by FTY720 and its effect on cell apoptosis	Int J Nanomedicine. 2018 Mar 5;13:1265-1280.
A549	100 nM	4 h	To evaluate the cellular uptake of LCP-II-siBeclin 1-FTY720 NPs	Int J Nanomedicine. 2018 Mar 5;13:1265-1280.

Cell Line

Panc05.04 cells BxPC3 and AsPC1 cells SMMC-7721 A549

Concentration

Treated Time

Description

References

Panc05.04 cells

5 µM

24 h

FTY-720 significantly inhibited the colony formation ability of SF3B1 K700E mutant Panc05.04 cells and reduced glucose uptake and lactate release.

Mol Oncol. 2021 Nov;15(11):3076-3090.

BxPC3 and AsPC1 cells

5 µM

24 h

FTY-720 did not significantly affect the glycolytic ability of BxPC3 and AsPC1 cells, but ectopic expression of SF3B1 K700E significantly promoted glucose uptake and lactate production.

Mol Oncol. 2021 Nov;15(11):3076-3090.

SMMC-7721

7.5 μM

24 h

To evaluate the autophagy induced by FTY720 and its effect on cell apoptosis

Int J Nanomedicine. 2018 Mar 5;13:1265-1280.

A549

100 nM

4 h

To evaluate the cellular uptake of LCP-II-siBeclin 1-FTY720 NPs

Int J Nanomedicine. 2018 Mar 5;13:1265-1280.

Fingolimod HCl/盐酸芬戈莫德动物实验

Species Mice Mice Mice Mice Mice Nude mice C57BL/6NCrl mice	Animal Model C57BL/6 mice Ccl19 -Cre × iDTR mice MC38, B16F10, CT26, 4T1 tumor models Nippostrongylus brasiliensis infection model Experimental Autoimmune Encephalomyelitis (EAE) model Pancreatic cancer xenograft model P. aeruginosa respiratory infection model	Administration	Dosage	Frequency	Description	References
Mice	C57BL/6 mice	Drinking water	2.5 mg/L	From 3 days prior to challenge and continued	To evaluate the effect of Fingolimod on CD8+ T cell recirculation, it was found that Fingolimod treatment delayed the protective response in s.c. vaccinated mice, but had little effect on virus control in combined vaccinated mice.	Front Immunol. 2023 Dec 18;14:1322536
Mice	Ccl19 -Cre × iDTR mice	Intraperitoneal injection	8 ng/g	Single injection, lasting 72 hours	Selective ablation of FRCs by DTxn injection to evaluate its impact on T cell and B cell responses. Results showed that ablation of FRCs led to significant reductions in T cell and B cell numbers and impaired antigen-specific T cell responses and humoral immunity.	Nat Immunol. 2014 Oct;15(10):973-81
Mice	MC38, B16F10, CT26, 4T1 tumor models	Subcutaneous injection	1.25 mg/kg or 10 mg/kg	Single administration, lasting 7 days	To study the effect of rhIL-7-hyFc treatment on CD8 TILs, the results showed that rhIL-7-hyFc significantly increased the number of PD-1/C0CD8 TILs and enhanced the antitumor efficacy of TCE immunotherapy.	Cell Rep Med. 2024 May 21;5(5):101567
Mice	Nippostrongylus brasiliensis infection model	Intraperitoneal injection	1 mg/kg	Daily, starting on the day of infection and continuing until the indicated time points	FTY720 significantly reduced the number of circulating ILC2s and decreased serum IL-13 levels during N. brasiliensis infection.	J Exp Med. 2020 Apr 6;217(4):e20191172
Mice	Experimental Autoimmune Encephalomyelitis (EAE) model	Oral	0.3 mg/kg	Once daily for 14 days	Evaluate the therapeutic effect of Fingolimod on the EAE model, results showed that Fingolimod significantly alleviated disease symptoms	PLoS Pathog. 2020 Aug 13;16(8):e1008679
Nude mice	Pancreatic cancer xenograft model	Intraperitoneal injection	3 mg/kg	Once daily for 1 month	FTY-720 significantly inhibited tumor growth of SF3B1 K700E-overexpressing Panc05.04-sh-SF3B1 cells but had no significant effect on SF3B1 WT Panc05.04-sh-SF3B1 cells.	Mol Oncol. 2021 Nov;15(11):3076-3090.
C57BL/6NCrl mice	P. aeruginosa respiratory infection model	Intraperitoneal injection	3 mg/kg	Twice daily for 7 days	To validate the function of the S1P1 receptor in P. aeruginosa infection, results showed that inhibition of S1P1 worsened the infection outcome	mBio. 2020 Mar 3;11(2):e00097-20

Species

Mice Mice Mice Mice Mice Nude mice C57BL/6NCrl mice

Animal Model

C57BL/6 mice Ccl19 -Cre × iDTR mice MC38, B16F10, CT26, 4T1 tumor models Nippostrongylus brasiliensis infection model Experimental Autoimmune Encephalomyelitis (EAE) model Pancreatic cancer xenograft model P. aeruginosa respiratory infection model

Administration

Dosage

Frequency

Description

References

Mice

C57BL/6 mice

Drinking water

2.5 mg/L

From 3 days prior to challenge and continued

To evaluate the effect of Fingolimod on CD8+ T cell recirculation, it was found that Fingolimod treatment delayed the protective response in s.c. vaccinated mice, but had little effect on virus control in combined vaccinated mice.

Front Immunol. 2023 Dec 18;14:1322536

Mice

Ccl19 -Cre × iDTR mice

Intraperitoneal injection

8 ng/g

Single injection, lasting 72 hours

Selective ablation of FRCs by DTxn injection to evaluate its impact on T cell and B cell responses. Results showed that ablation of FRCs led to significant reductions in T cell and B cell numbers and impaired antigen-specific T cell responses and humoral immunity.

Nat Immunol. 2014 Oct;15(10):973-81

Mice

MC38, B16F10, CT26, 4T1 tumor models

Subcutaneous injection

1.25 mg/kg or 10 mg/kg

Single administration, lasting 7 days

To study the effect of rhIL-7-hyFc treatment on CD8 TILs, the results showed that rhIL-7-hyFc significantly increased the number of PD-1/C0CD8 TILs and enhanced the antitumor efficacy of TCE immunotherapy.

Cell Rep Med. 2024 May 21;5(5):101567

Mice

Nippostrongylus brasiliensis infection model

Intraperitoneal injection

1 mg/kg

Daily, starting on the day of infection and continuing until the indicated time points

FTY720 significantly reduced the number of circulating ILC2s and decreased serum IL-13 levels during N. brasiliensis infection.

J Exp Med. 2020 Apr 6;217(4):e20191172

Mice

Experimental Autoimmune Encephalomyelitis (EAE) model

Oral

0.3 mg/kg

Once daily for 14 days

Evaluate the therapeutic effect of Fingolimod on the EAE model, results showed that Fingolimod significantly alleviated disease symptoms

PLoS Pathog. 2020 Aug 13;16(8):e1008679

Nude mice

Pancreatic cancer xenograft model

Intraperitoneal injection

3 mg/kg

Once daily for 1 month

FTY-720 significantly inhibited tumor growth of SF3B1 K700E-overexpressing Panc05.04-sh-SF3B1 cells but had no significant effect on SF3B1 WT Panc05.04-sh-SF3B1 cells.

Mol Oncol. 2021 Nov;15(11):3076-3090.

C57BL/6NCrl mice

P. aeruginosa respiratory infection model

Intraperitoneal injection

3 mg/kg

Twice daily for 7 days

To validate the function of the S1P1 receptor in P. aeruginosa infection, results showed that inhibition of S1P1 worsened the infection outcome

mBio. 2020 Mar 3;11(2):e00097-20

Fingolimod HCl/盐酸芬戈莫德动物研究

Dose

Mice: 1 mg/kg - 10 mg/kg^[5] (i.p.), 0.03 mg/kg - 1 mg/kg^[4] (p.o.) Rat: 3 mg/kg - 7.5 mg/kg^[6] (i.v.)

Administration

i.p., p.o., i.v.

Pharmacokinetics

Animal	Mice^[6]	Rats^[6]	Dogs^[6]	Monkeys^[6]
Dose	2.5 mg/kg (p.o. or i.v.)	7.5 mg/kg (p.o.) 4 mg/kg (i.v.)	3 mg/kg (p.o.) 1 mg/kg (i.v.)	3 mg/kg (p.o.) 0.1 mg/kg (i.v.)
Administration	p.o. i.v.	p.o. i.v.	p.o. i.v.
F	66% (p.o.)	59% (p.o.)	60.8% (p.o.)	51% (p.o.)
T_1/2	25 h (p.o.)		29.3 h (p.o.)
T_max	8 h (p.o.)	8 h (p.o.)	9.3 h (p.o.)	9.3 h (p.o.)
MRT	31.5 h (i.v.)	32 h (p.o.)	34.7 h (i.v.)
t_1/2β			24.6 h (i.v.)
T_1/2β	27.8 h (i.v.)
C_max	95.3 ng/ml (p.o.)	148 ng/ml (p.o.)	165 ng/ml (p.o.)	30.7 ng/ml (p.o.)
CL	0.55 L/h/kg (i.v.) 9.17 ml/min/kg (i.v.)	0.666 L/h/kg (i.v.) 11.1 ml/min/kg (i.v.)	0.219 L/h/kg (i.v.) 3.65 ml/min/kg (i.v.)	0.0917 L/h/kg (i.v.) 1.528 ml/min/kg (i.v.)
Vss	17.30 L/kg (i.v.)	21 L/kg (p.o.)	7.60 L/kg (i.v.)	17.3 L/kg (i.v.)
AUC	3167 ng·h/ml (p.o.) 5442 ng·h/ml (i.v.)	6795 ng·h/ml (p.o.) 6027 ng·h/ml (i.v.)	8491 ng·h/ml (p.o.) 4658 ng·h/ml (i.v.)	1640 ng·h/ml (p.o.) 323 ng·h/ml (i.v.)

Fingolimod HCl/盐酸芬戈莫德参考文献

Fingolimod HCl/盐酸芬戈莫德实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.54mL

2.91mL

1.45mL

29.08mL

5.82mL

2.91mL

Fingolimod HCl/盐酸芬戈莫德技术信息

CAS号	162359-56-0
分子式	C₁₉H₃₄ClNO₂
分子量	343.93
SMILES Code	OCC(CCC1=CC=C(CCCCCCCC)C=C1)(N)CO.[H]Cl
MDL No.	MFCD00939512

别名	芬戈莫德盐酸盐 ;FTY720; Fingolimod (hydrochloride); Fingolimod HCl
运输	蓝冰
InChI Key	SWZTYAVBMYWFGS-UHFFFAOYSA-N
Pubchem ID	107969

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(305.29 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 50 mg/mL(145.38 mM)，配合低频超声助溶

无水乙醇: 100 mg/mL(290.76 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

CHO cells		Function assay		Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells, IC50=0.84 μM.	15615513
human BLIN-1 cells		Cytotoxic assay	72 h	Cytotoxicity against Ph-negative human BLIN-1 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=5.5 μM.	24273632
human BV173 cells		Cytotoxic assay	72 h	Cytotoxicity against Ph-positive human BV173 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.3 μM.	24273632
human CCRF-CEM cells		Cytotoxic assay	72 h	Cytotoxicity against Ph-negative human CCRF-CEM cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.8 μM.	24273632
human DU145 cells		Cytotoxic assay	72 h	Cytotoxicity against human DU145 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.5 μM.	24273632
human HCT116 cells		Proliferation assay	78 h	Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5 μM.	21456524
human Jurkat cells		Function assay	18 h	Reversal of inhibition of mitochondrial function in human Jurkat cells after 18 hrs in presence of Z-VAD-fmk	17400555
human MCF7 cells		Proliferation assay	78 h	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5 μM.	21456524
human NALM6 cells		Cytotoxic assay	72 h	Cytotoxicity against Ph-negative human NALM6 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=9.6 μM.	24273632
human PC3 cells		Cytotoxic assay	72 h	Cytotoxicity against human PC3 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=9.8 μM.	24273632
human SK-BR-3 cells		Proliferation assay	78 h	Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50= 5 μM.	21456524
human SUP-B15 cells		Cytotoxic assay	72 h	Cytotoxicity against Ph-positive human SUP-B15 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.8 μM.	24273632
human SW620 cells		Proliferation assay	78 h	Antiproliferative activity against human SW620 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5 μM.	21456524
human U2OS cells		Function assay		Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining, EC50=0.002 μM.	22104144
MDA-MB-231 cells		Proliferation assay	78 h	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50= 5 μM.	21456524
mouse bone marrow cells		Cytotoxic assay	72 h	Cytotoxicity against BCR-ABL fusion protein 190 expressing mouse bone marrow cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=3.3 μM.	24273632
mouse MN9D cells	0.16 μM	Function assay	72 h	Neuroprotective activity in mouse MN9D cells assessed as blocking of TNF-alpha associated toxicity at 0.16 uM after 72 hrs by Trypan blue staining.	25050165
mouse MN9D cells	0.16 μM	Function assay	24 h	Neuroprotective activity in mouse MN9D cells assessed as stimulation of BDNF expression at 0.16 uM after 24 hrs	25050165
mouse MN9D cells	5 μM	Function assay		Induction of PP2A catalytic subunit activity in mouse MN9D cells assessed as phosphate level at 5 uM	25050165
rat PC12 cells	5 μM	Function assay	30 to 120 mins	Induction of PP2A catalytic subunit activity in rat PC12 cells assessed as phosphate level at 5 uM measured 30 to 120 mins.	25050165
Sf9 insect cells		Function assay	1 h	Inhibition of human recombinant S1PL (62 to 568) expressed in Sf9 insect cells using S1P as substrate after 1 hr	24809814

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