首页 工具
登录
购物车
Ponesimod

Ponesimod

产品编号 T3258   CAS 854107-55-4
别名: ACT-128800

Ponesimod (ACT-128800) 是一种选择性 S1P1可口服激动剂,在放射性配体结合试验中的 IC50值为 6 nM。它可高效激活 S1P1介导的信号转导,EC50为5.7 nM。它可预防淋巴细胞介导的组织炎症,具有潜在的免疫调节活性。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
Ponesimod Chemical Structure
Ponesimod, CAS 854107-55-4
规格 价格/CNY 货期 数量
1 mg ¥ 368 现货
2 mg ¥ 527 现货
5 mg ¥ 813 现货
10 mg ¥ 1,330 现货
25 mg ¥ 2,230 现货
50 mg ¥ 3,330 现货
100 mg ¥ 4,850 现货
500 mg ¥ 9,870 现货
1 mL * 10 mM (in DMSO) ¥ 913 现货
产品目录号及名称: Ponesimod (T3258)
点击图片重新获取验证码
选择批次  
纯度: 99.42%
纯度: 98.22%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.
靶点活性 S1P1 receptor:5.7 nM(EC50)
体外活性 Relative to the potency of S1P, the potency of ponesimod at human recombinant receptors was 4.4-fold higher for S1P1 and 150-fold lower for human S1P3. Therefore, ponesimod was ~650-fold more selective for human S1P1 over S1P3 than the natural ligand[1].
体内活性 Ponesimod is a new, potent, and selective S1P1 receptor agonist with pharmacokinetic properties allowing rapid restoration of lymphocyte count in peripheral blood upon discontinuation. Ponesimod prevents edema formation, inflammatory cell accumulation, and cytokine release in the skin of mice with delayed-type hypersensitivity. Ponesimod also prevents the increase in paw volume and joint inflammation in rats with adjuvant-induced arthritis. Selective activation of S1P1 using ponesimod leads to blood lymphocyte count reduction and prevention in models of lymphocyte-mediated tissue inflammation. It has the potential to be as effective in animal models of autoimmunity and human autoimmune disease via its effect on T and B cell blood count. Thus, ponesimod may represent a new therapeutic option for the treatment of autoimmune diseases[1]. Ponesimod is eliminated within 1 week of discontinuation and its pharmacological effects are rapidly reversible [2].
激酶实验 The enzymatic reactions are conducted in duplicate at room temperature for 1 hour in a 50 μL mixture containing PKMT assay buffer, substrate coated plate, 10 M SAM, a HMT enzyme (EZH2 (800 ng/reaction), MLL (300 ng/reaction), PRMT1 (0.5 ng/reaction), SUV39H1 (75 ng/reaction) and UNC0638 (0-1.25 μM). After enzymatic reactions, 100 μL of first antibody is added to each well and the plate is incubated at room temperature for an additional 1 h. 100 μL of secondary antibody is added to each well and the plate is incubated at room temperature for an additional 30 min. 100 μL of developer reagents are added to wells and luminescence is measured using a BioTek SynergyTM 2 microplate reader. Enzyme activity assays are performed in duplicates at each concentration. The luminescence data are analyzed using the computer software, Graphpad Prism[1].
别名 ACT-128800
分子量 460.97
分子式 C23H25ClN2O4S
CAS No. 854107-55-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (119.31 mM)

Ethanol: 92 mg/mL (199.58 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.1693 mL 10.8467 mL 21.6934 mL 54.2335 mL
5 mM 0.4339 mL 2.1693 mL 4.3387 mL 10.8467 mL
10 mM 0.2169 mL 1.0847 mL 2.1693 mL 5.4233 mL
20 mM 0.1085 mL 0.5423 mL 1.0847 mL 2.7117 mL
50 mM 0.0434 mL 0.2169 mL 0.4339 mL 1.0847 mL
100 mM 0.0217 mL 0.1085 mL 0.2169 mL 0.5423 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Piali L. et al. J Pharmacol Exp Ther. 2011, 337(2):547-556. 2. D'Ambrosio D, et al. Ther Adv Chronic Dis. 2016, 7(1):18-33. 3. Fauzyah Y, Ono C, Torii S, et al. Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation[J]. Antiviral Research. 2020: 104999.

文献引用

1. Fauzyah Y, Ono C, Torii S, et al. Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation. Antiviral Research. 2021 Feb;186:104999
CYM-5541 CYM5442 S1p receptor agonist 1 SK1-IN-1 MHP ML-031 4-Deoxypyridoxine hydrochloride Siponimod

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌上市药物库 神经退行性疾病化合物库 抗癌临床化合物库 临床期小分子药物库 抑制剂库 已知活性化合物库 口服活性化合物库 血脑屏障通透化合物库 抗肥胖化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ponesimod 854107-55-4 GPCR/G Protein S1P Receptor LPL Receptor S1P1 Lysophospholipid Receptor inflammation Inhibitor inhibit ACT-128800 ACT128800 lymphocyte-mediated ACT 128800 inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼