Ponesimod | ACT-128800 | S1P1 Agonist | AmBeed-信号通路专用抑制剂

Ponesimod {[allProObj[0].p_purity_real_show]}

货号：A257238 同义名： ACT-128800

Ponesimod 是一种口服活性的 S1P1 受体激动剂（EC₅₀ = 5.7 nM），用于多发性硬化症（MS）及银屑病的研究。

Ponesimod 化学结构
CAS号：854107-55-4

Ponesimod 3D分子结构
CAS号：854107-55-4

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Ponesimod 生物活性

描述

S1P is a signaling lipid that regulates many cellular processes in mammals^[3]. Ponesimod is a potent, selective, and orally active S1P(1) receptor agonist (IC50=6nM) selected for clinical development^[4]. Ponesimod activated S1P(1)-mediated signal transduction with high potency (EC50-5.7nM) and selectively. Oral administration of ponesimod (3-100mg/kg) to rats led to a dose-dependent decrease of blood lymphocyte count. Ponesimod (30 mg/kg) also prevents footpad swelling in a rat model of adjuvant-induced arthritis^[5].

Ponesimod 细胞实验

Cell Line Primary microglia Hela cells BV2 cells Mixed glial cells Human primary astrocytes Human primary astrocytes C6 glioblastoma cells Hela cells BV2 cells Primary glial cells Human primary astrocytes Human primary astrocytes C6 glioblastoma cells	Concentration	Treated Time	Description	References
Primary microglia	100 nM	24 hours	Ponesimod enhanced phagocytosis of Aβ42 in microglia.	EBioMedicine. 2023 Aug;94:104713.
Hela cells	100 nM	4 hours	Ponesimod reduced the Aβ42-induced formation of the TLR4-S1PR1 complex.	EBioMedicine. 2023 Aug;94:104713.
BV2 cells	10 nM or 100 nM	24 hours	Ponesimod increased the phagocytosis of Aβ42 in BV2 cells.	EBioMedicine. 2023 Aug;94:104713.
Mixed glial cells	10 nM or 100 nM	24 hours	Ponesimod prevented the Aβ42-induced increase in TLR4 and S1PR1 levels, as well as the formation of their complex.	EBioMedicine. 2023 Aug;94:104713.
Human primary astrocytes	1 µM	24 or 48 hours	Evaluate the effect of Ponesimod on cytokine-induced gene expression changes. Results showed Ponesimod significantly downregulated genes related to neuroinflammation.	FASEB J. 2022 Feb;36(2):e22132.
Human primary astrocytes	1 µM	1 hour	Assess the effect of Ponesimod on S1P1 internalization. Results showed Ponesimod induced S1P1 internalization.	FASEB J. 2022 Feb;36(2):e22132.
C6 glioblastoma cells	1 µM	1 hour	Evaluate the selectivity of Ponesimod for S1PR internalization. Results showed Ponesimod only reduced cell surface expression of S1P1, while other S1PRs remained unchanged.	FASEB J. 2022 Feb;36(2):e22132.
Hela cells	100 nM	4 hours	Ponesimod reduced the Aβ42-induced formation of TLR4-S1PR1 complex.	EBioMedicine. 2023 Aug;94:104713.
BV2 cells	10 nM or 100 nM	24 hours	10 nM Ponesimod increased phagocytosis of Aβ42 in BV2 cells, while 100 nM had no significant effect.	EBioMedicine. 2023 Aug;94:104713.
Primary glial cells	10 nM or 100 nM	24 hours	Ponesimod prevented the Aβ42-induced increase in TLR4 and S1PR1 levels and their complex formation.	EBioMedicine. 2023 Aug;94:104713.
Human primary astrocytes	1 µM	18 hours	Evaluate the effect of Ponesimod on S1P-induced Ca2+ signaling. Results showed Ponesimod effectively blocked S1P-induced Ca2+ signals.	FASEB J. 2022 Feb;36(2):e22132.
Human primary astrocytes	1 µM	1 hour	Visualize Ponesimod-induced S1P1 internalization by transfecting a S1P1-EGFP fusion gene. Results showed Ponesimod effectively induced S1P1 internalization.	FASEB J. 2022 Feb;36(2):e22132.
C6 glioblastoma cells	1 µM	1 hour	Evaluate the selective effect of Ponesimod on S1PR internalization. Results showed Ponesimod only reduced the cell surface expression of S1P1, while S1P affected multiple S1PR subtypes.	FASEB J. 2022 Feb;36(2):e22132.

Cell Line

Concentration

Treated Time

Description

References

Primary microglia

100 nM

24 hours

Ponesimod enhanced phagocytosis of Aβ42 in microglia.

EBioMedicine. 2023 Aug;94:104713.

Hela cells

100 nM

4 hours

Ponesimod reduced the Aβ42-induced formation of the TLR4-S1PR1 complex.

EBioMedicine. 2023 Aug;94:104713.

BV2 cells

10 nM or 100 nM

24 hours

Ponesimod increased the phagocytosis of Aβ42 in BV2 cells.

EBioMedicine. 2023 Aug;94:104713.

Mixed glial cells

10 nM or 100 nM

24 hours

Ponesimod prevented the Aβ42-induced increase in TLR4 and S1PR1 levels, as well as the formation of their complex.

EBioMedicine. 2023 Aug;94:104713.

Human primary astrocytes

1 µM

24 or 48 hours

Evaluate the effect of Ponesimod on cytokine-induced gene expression changes. Results showed Ponesimod significantly downregulated genes related to neuroinflammation.

FASEB J. 2022 Feb;36(2):e22132.

Human primary astrocytes

1 µM

1 hour

Assess the effect of Ponesimod on S1P1 internalization. Results showed Ponesimod induced S1P1 internalization.

FASEB J. 2022 Feb;36(2):e22132.

C6 glioblastoma cells

1 µM

1 hour

Evaluate the selectivity of Ponesimod for S1PR internalization. Results showed Ponesimod only reduced cell surface expression of S1P1, while other S1PRs remained unchanged.

FASEB J. 2022 Feb;36(2):e22132.

Hela cells

100 nM

4 hours

Ponesimod reduced the Aβ42-induced formation of TLR4-S1PR1 complex.

EBioMedicine. 2023 Aug;94:104713.

BV2 cells

10 nM or 100 nM

24 hours

10 nM Ponesimod increased phagocytosis of Aβ42 in BV2 cells, while 100 nM had no significant effect.

EBioMedicine. 2023 Aug;94:104713.

Primary glial cells

10 nM or 100 nM

24 hours

Ponesimod prevented the Aβ42-induced increase in TLR4 and S1PR1 levels and their complex formation.

EBioMedicine. 2023 Aug;94:104713.

Human primary astrocytes

1 µM

18 hours

Evaluate the effect of Ponesimod on S1P-induced Ca2+ signaling. Results showed Ponesimod effectively blocked S1P-induced Ca2+ signals.

FASEB J. 2022 Feb;36(2):e22132.

Human primary astrocytes

1 µM

1 hour

Visualize Ponesimod-induced S1P1 internalization by transfecting a S1P1-EGFP fusion gene. Results showed Ponesimod effectively induced S1P1 internalization.

FASEB J. 2022 Feb;36(2):e22132.

C6 glioblastoma cells

1 µM

1 hour

Evaluate the selective effect of Ponesimod on S1PR internalization. Results showed Ponesimod only reduced the cell surface expression of S1P1, while S1P affected multiple S1PR subtypes.

FASEB J. 2022 Feb;36(2):e22132.

Ponesimod 动物实验

Species C57BL/6J male mice 5XFAD mice	Animal Model Cuprizone-induced demyelination model Alzheimer's disease model	Administration	Dosage	Frequency	Description	References
C57BL/6J male mice	Cuprizone-induced demyelination model	Oral	30 mg/kg	Twice daily for 5–6 weeks	Evaluate the protective effect of Ponesimod against demyelination. Results showed Ponesimod selectively protected the cingulum from demyelination and increased oligodendrocyte numbers.	FASEB J. 2022 Feb;36(2):e22132.
5XFAD mice	Alzheimer's disease model	Oral gavage	30 mg/kg	Once daily for 4 weeks	Ponesimod reduced neuroinflammation, improved spatial memory, and decreased the number and size of amyloid plaques.	EBioMedicine. 2023 Aug;94:104713.

Species

C57BL/6J male mice 5XFAD mice

Animal Model

Cuprizone-induced demyelination model Alzheimer's disease model

Administration

Dosage

Frequency

Description

References

C57BL/6J male mice

Cuprizone-induced demyelination model

Oral

30 mg/kg

Twice daily for 5–6 weeks

Evaluate the protective effect of Ponesimod against demyelination. Results showed Ponesimod selectively protected the cingulum from demyelination and increased oligodendrocyte numbers.

FASEB J. 2022 Feb;36(2):e22132.

5XFAD mice

Alzheimer's disease model

Oral gavage

30 mg/kg

Once daily for 4 weeks

Ponesimod reduced neuroinflammation, improved spatial memory, and decreased the number and size of amyloid plaques.

EBioMedicine. 2023 Aug;94:104713.

Ponesimod 临床研究

NCT号

适应症或疾病

临床期

招募状态

预计完成时间

地点

NCT01208090

Psoriasis

Phase 2

Completed

NCT01006265

Multiple Sclerosis

Phase 2

Completed

NCT02223832

Healthy

Phase 1

Completed

United States, Hawaii ... 展开 >> Hawaii Clinical Research Center Honolulu, Hawaii, United States, 96813 收起 <<

Ponesimod 参考文献

Ponesimod 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.85mL

2.17mL

1.08mL

21.69mL

4.34mL

2.17mL

Ponesimod 技术信息

CAS号	854107-55-4
分子式	C₂₃H₂₅ClN₂O₄S
分子量	460.97
SMILES Code	O=C1N(C2=CC=CC=C2C)/C(S/C1=C\C3=CC=C(OC[C@H](O)CO)C(Cl)=C3)=N/CCC
MDL No.	MFCD18207776

别名	ACT-128800
运输	蓝冰
InChI Key	LPAUOXUZGSBGDU-ULCCENQXSA-N
Pubchem ID	11363176

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(227.78 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

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

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01208090	Psoriasis	Phase 2	Completed	-	-
NCT01006265	Multiple Sclerosis	Phase 2	Completed	-	-
NCT02223832	Healthy	Phase 1	Completed	-	United States, Hawaii ... 展开 >> Hawaii Clinical Research Center Honolulu, Hawaii, United States, 96813 收起 <<
NCT02068235	Healthy	Phase 1	Completed	-	United Kingdom ... 展开 >> Simbec Research Limited Merthyr Tydfil, United Kingdom, CF48 4DR 收起 <<
NCT02126956	Pharmacokinetics	Phase 1	Completed	-	Switzerland ... 展开 >> Swiss Pharma Contract Allschwil, Switzerland 收起 <<
NCT02029482	Safety and Tolerability	Phase 1	Completed	-	United Kingdom ... 展开 >> Quintiles Drug Research Unit at Guyʼs Hospital London, United Kingdom, SE1 1YR 收起 <<
NCT02907177	Multiple Sclerosis	Phase 3	Recruiting	March 31, 2020	-
NCT01093326	Multiple Sclerosis	Phase 2	Active, not recruiting	December 15, 2021	-
NCT02425644	Multiple Sclerosis	Phase 3	Active, not recruiting	May 15, 2019	-
NCT03232073	Multiple Sclerosis	Phase 3	Enrolling by invitation	April 2, 2022	-
NCT00852670	Plaque Psoriasis	Phase 2	Completed	-	Austria ... 展开 >> Landeskrankenhaus - Universitätsklilnikum Graz, Allgemeine Dermatologie Graz, Austria, 8036 University Klinik of Vienna Vienna, Austria, 1090 France Departement de Pneumologie/ Unité Immunologie Clinique Allergie- Centre Hospitalier Lyon sud Lyon, France, 69000 CHU de Nice-Hôpital de l'Archet 2 / Service de dermatologie Nice, France, 6202 Dermatologie, Hôpital Purpan Universtité Paul Sabatier Toulouse, France, 31000 Germany Klinik für Dermatologie Venerologie und Allergologie Berlin, Germany, 10117 Universitätsklinikum Hamburg-Eppendorf Hamburg, Germany, 20246 Department of Dermatology University Hospital Johannes Gutenberg-University Mainz Mainz, Germany, 55131 University Clinic Münster Clinic and Policlinic for skin diseases Muenster, Germany, 48149 Hungary Semmelweis Universtity Dept. dermato-venerology and skin oncology Budapest, Hungary, 1085 UNIVERSITY OF DEBRECEN Department of dermatology Debrecen, Hungary, 4012 University of Szeged Department of dermatology and allergology Szeged, Hungary, 6720 Veszprem County Csolnoky Ferenc Hospital Dermatology Department Veszprem, Hungary, 8200 Serbia Clinical Centre of Nis Clinic of Dermato-venerology Nis, Serbia, 18000 收起 <<
NCT02136888	Healthy	Phase 1	Completed	-	United States, Indiana ... 展开 >> Covance Clinical Research Unit (CRU) Evansville, Indiana, United States, 47710 收起 <<
NCT02461134	Chronic Graft Versus Host Dise... 展开 >>ase 收起 <<	Phase 2	Terminated(Low recruitment)	-	United States, Arizona ... 展开 >> Virginia Piper Cancer Institute Scottsdale, Arizona, United States, 85258 United States, California Moore Cancer Center - UCSD La Jolla, California, United States, 92093 David Geffen School of Med at UCLA Los Angeles, California, United States, 90095 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Indiana Indiana University Simon Cancer Center Indianapolis, Indiana, United States, 46202 United States, Maryland National Cancer Institute Bethesda, Maryland, United States, 20892-1203 United States, Minnesota University of Minnesota - Masonic Cancer CTR CLIN TRIALS CTR Minneapolis, Minnesota, United States, 55455 United States, Missouri Washington Univ School of Med, Oncology (St.Louis) Saint Louis, Missouri, United States, 63110 United States, New York Stony Brook Univ. Medical Center Stony Brook, New York, United States, 11794 United States, Washington Fred Hutchinson Cancer Res CTR Seattle, Washington, United States, 98109-1023 收起 <<
NCT02461134	-		Terminated(Low recruitment)	-	-

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Ponesimod 动物实验

Ponesimod 临床研究

Ponesimod 参考文献

Ponesimod 实验方案

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最近浏览的产品

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摩尔计算器

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总药量计算器

工作液计算器

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