Ponesimod
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EC50为5.7 nM。
Ponesimod是鞘氨醇-1-磷酸受体1(S1P1)调节剂。
据报道,淋巴细胞从淋巴结排出及其再循环进入血液由S1P控制。五种S1P受体之一S1P1是介导淋巴细胞排出的细胞受体。因此,S1P1的非选择性激动剂导致血液淋巴细胞计数减少。
体外:先前的研究发现,ponesimod可以强效激活S1P1介导的信号转导。此外,相对于对S1P的效力,Ponesimod对人重组受体的效力为,对S1P1高4.4倍,对人S1P3低150倍。因此,相比内源性配体,ponesimod对人S1P1的选择性比S1P3高650倍[1]。
体内:动物研究显示,大鼠口服给药ponesimod导致血液淋巴细胞计数剂量依赖性的降低,并且在停止ponesimod治疗后48h内血液淋巴细胞计数回到基线。此外,ponesimod在具有延迟型超敏反应的小鼠皮肤中预防炎症细胞积累、水肿形成,以及细胞因子释放。此外,在佐剂诱导的关节炎大鼠中,ponesimod还可以防止爪体积和关节炎症的增加[2]。
临床试验:临床数据显示出ponesimod剂量依赖性的治疗效果、可接受的安全性和耐受性。此外,II期临床数据还显示出ponesimod在牛皮癣中的治疗功效[2]。
参考文献:
[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.
Storage | Store at -20°C |
M.Wt | 460.97 |
Cas No. | 854107-55-4 |
Formula | C23H25ClN2O4S |
Solubility | Soluble in DMSO |
Chemical Name | (2E,5Z)-5-(3-chloro-4-((S)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one |
SDF | Download SDF |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |