1. GPCR/G Protein
  2. LPL Receptor
  3. Ponesimod

Ponesimod (Synonyms: ACT-128800)

目录号: HY-10569 纯度: 99.81%
产品使用指南

Ponesimod (ACT-128800) 是一种有效的,具有选择性和口服活性的 S1P1 的激动剂,在放射性配体结合试验中的 IC50 值为 6 nM。Ponesimod 可高效激活 S1P1 介导的信号转导 (EC50=5.7 nM)。Ponesimod 可以预防淋巴细胞介导的组织炎症。

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Ponesimod Chemical Structure

Ponesimod Chemical Structure

CAS No. : 854107-55-4

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10 mM * 1 mL in DMSO ¥1100
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation[1][2][3].

IC50 & Target

S1PR1

6 nM (IC50)

S1PR3

2068 nM (IC50)

S1PR4

1956 nM (IC50)

S1PR5

142 nM (IC50)

体外研究
(In Vitro)

Ponesimod activates human S1P1-5 receptors with EC50s of 5.7, >10000, 105, 1108 and 59.1 nM respectively in GTPγS binding assay[2].
Ponesimod activates S1P1 receptors with EC50s of 5.7, 1.9, and 1.4 nM for human, rat, and mouse S1P receptors respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ponesimod (30 and 175 mg/kg; once daily p.o. for 8 d) prevents delayed-type hypersensitivity in mice[2].
Ponesimod (30 mg/kg by gavage 3 h before and 6 h after adjuvant injection followed by 100 mg/kg/day by administration as food admix for 18 days) prevents adjuvant-induced arthritis in rats[2].
Ponesimod (0.3-100 mg/kg; a single oral gavage) causes a dose-dependent reduction in lymphocyte count, with a plateau effect being reached at 3 mg/kg in rats[2].
Ponesimod (100 mg/kg; once daily oral gavage for 7 d) results in a lymphocyte count reduction to 1900 lymphocytes/μL, and this effect is maintained over the entire 7 days studies. Lymphocyte count returned to baseline levels within 48 h after discontinuation of dosing[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (15-25 g) sensitized with DNFB[2]
Dosage: 30 and 175 mg/kg
Administration: Gavage (30 mg/kg) 19 and 3 h before sensitization, followed by administration as food admix (175 mg/kg/day) for 8 days
Result: Caused a 60 to 90% reduction of delayed-type hypersensitivity (DTH) parameters of the skin, such as edema, protein extravasation, and neutrophil myeloperoxidase (MPO) activity.
Reduced skin levels of proinflammatory cytokines, such as IL-1β, IL-6, IFNγ, TNFα, and several chemokines to different degrees ranging from -27 to -100%.
Clinical Trial
分子量

460.97

Formula

C23H25ClN2O4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (216.93 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1693 mL 10.8467 mL 21.6934 mL
5 mM 0.4339 mL 2.1693 mL 4.3387 mL
10 mM 0.2169 mL 1.0847 mL 2.1693 mL
*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.42 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.42 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

纯度: 99.81%

  • 摩尔计算器

  • 稀释计算器

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HY-10569
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