Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (119.31 mM)
Ethanol: 92 mg/mL (199.58 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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