Ponesimod
(Synonyms: ACT-128800) 目录号 : GC16660
A potent S1P1 receptor agonist
Cas No.:854107-55-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
EC50: 5.7 nM
Ponesimod is a sphingosine-1-phosphate receptor 1 (S1P1) modulator.
Lymphocyte exit from lymph nodes and its recirculation into blood is reported to be controlled by S1P. The cellular receptor mediating lymphocyte exit is one of five S1P receptors, S1P1. Thus, the nonselective agonists for S1P1 lead to blood lymphocyte count reduction.
In vitro: Previous study found that ponesimod could activate S1P1-mediated signal transduction with high potency. Moreover, relative to the potency for S1P, the potency of ponesimod at human recombinant receptors was 4.4-fold higher for S1P1 and 150-fold lower for human S1P3. Thus, ponesimod was 650-fold more selective for human S1P1 over S1P3 than the endogeneous ligand [1].
In vivo: Animal study showed that the oral administration of ponesimod to rats resulted in a dose-dependent decrease of blood lymphocyte count, and the blood lymphocyte count returned to baseline within 48 h after discontinuation of ponesimod treatment. In addition, ponesimod prevented inflammatory cell accumulation, edema formation, as well as cytokine release in the skin of mice with delayed-type hypersensitivity. Furthermore, in rats with adjuvant-induced arthritis, ponesimod could also prevent the increase in paw volume and joint inflammation [2].
Clinical trial: Clinical data have shown a dose-dependent therapeutic effect of ponesimod, acceptable safety and tolerability. Furthermore, phase II clinical data have also shown therapeutic efficacy of ponesimod in psoriasis [2].
References:
[1] Piali L, Froidevaux S, Hess P, Nayler O, Bolli MH, Schlosser E, Kohl C, Steiner B, Clozel M. The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation. J Pharmacol Exp Ther. 2011 May;337(2):547-56.
[2] D'Ambrosio D, Freedman MS, Prinz J. Ponesimod, a selective S1P1 receptor modulator: a potential treatment for multiple sclerosis and other immune-mediated diseases. Ther Adv Chronic Dis. 2016 Jan;7(1):18-33.
| Cas No. | 854107-55-4 | SDF | |
| 别名 | ACT-128800 | ||
| 化学名 | (2E,5Z)-5-(3-chloro-4-((S)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one | ||
| Canonical SMILES | O=C1N(C2=CC=CC=C2C)/C(S/C1=C\C3=CC=C(OC[C@@H](O)CO)C(Cl)=C3)=N\CCC | ||
| 分子式 | C23H25ClN2O4S | 分子量 | 460.97 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 5 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。