Ponesimod ACT-128800|cas:854107-55-4|西域试剂

Ponesimod ACT-128800,99.81%

产品编号：Bellancom-10569| CAS NO：854107-55-4| 分子式：C₂₃H₂₅ClN₂O₄S| 分子量：460.97

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货号	价格	库存与货期
Bellancom-10569	￥1000.00	杭州北京（现货）
Bellancom-10569	￥1600.00	杭州北京（现货）
Bellancom-10569	￥5200.00	杭州北京（现货）
Bellancom-10569	￥8500.00	杭州北京（现货）

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Ponesimod ACT-128800

产品介绍

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。

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.

体外研究

Ponesimod activates human S1P_1-5 receptors with EC₅₀s of 5.7, >10000, 105, 1108 and 59.1 nM respectively in GTPγS binding assay.
Ponesimod activates S1P₁ receptors with EC₅₀s of 5.7, 1.9, and 1.4 nM for human, rat, and mouse S1P receptors respectively.

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

体内研究

Ponesimod (30 and 175 mg/kg; once daily p.o. for 8 d) prevents delayed-type hypersensitivity in mice.
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.
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.
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.

西域 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
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%.

体内研究

西域 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
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%.

性状

Solid

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。