Ozanimod (RPC1063)
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.
Ozanimod(RPC1063)是鞘氨醇-1-磷酸受体亚型1(S1P 1)和5(S1P5)的高口服生物可利用激动剂。S1P受体属于G蛋白偶联受体家族,含有5个亚型,为 S1P1-5。S1P受体参与冠状动脉口径、内皮完整性、心功能和淋巴细胞再循环[1]。
体外实验:Ozanimod(RPC1063)是S1P1和S1P5受体的特异性激动剂。对S1P1受体cAMP的产生和[35S]-GTPγS结合的EC50值分别为160 ± 60 pM和410 ± 160 pM。Ozanimod对S1P5受体的83%Emax值为11 ± 4.3 nM。含S1P1受体的HEK293T细胞经过10 nM浓度的RPC1063培养1小时后,RPC1063剂量依赖性的降低了S1P1受体在细胞表面上的重表达,并导致S1P1受体在细胞膜上表达的持续损失[1]。
在体实验:在小鼠和大鼠中,口服Ozanimod的T1/2分别为4.7小时和5.1小时。给药6小时后,T淋巴细胞循环下降约81-82%,大鼠和小鼠的最大血药浓度分别为45 nM和159 nM。口服剂量为0.2或0.6 mg/kg/day 的ozanimod剂量依赖性的降低了小鼠的疾病评分[1]。
临床试验:在双盲、安慰剂对照的中度至重度溃疡性结肠炎患者的2期临床试验中,1 mg 的ozanimod治疗8周后,57%的患者发生临床反应,而0.5mg 的ozanimod造成了54%的响应。在第32周,1 mg和0.5 mg剂量所对应的临床缓解率为21%和26%。副作用主要是贫血和头痛[2]。
参考文献:
Scott F L, Clemons B, Brooks J, et al. Ozanimod (RPC1063) is a potent sphingosine‐1‐phosphate receptor‐1 (S1P1) and receptor‐5 (S1P5) agonist with autoimmune disease‐modifying activity[J]. British Journal of Pharmacology, 2016.
Sandborn WJ, Feagan BG1, et al. Ozanimod Induction and Maintenance Treatment for Ulcerative Colitis. N Engl J Med. 2016, 374(18):1754-1762.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 404.46 |
Cas No. | 1306760-87-1 |
Formula | C23H24N4O3 |
Solubility | ≥40.4 mg/mL in DMSO; insoluble in H2O; ≥2.25 mg/mL in EtOH with ultrasonic |
Chemical Name | (S)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1H-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile |
SDF | Download SDF |
Canonical SMILES | CC(OC1=C(C#N)C=C(C2=NC(C3=CC=CC4=C3CC[C@]4([H])NCCO)=NO2)C=C1)C |
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。 |
质量控制和MSDS
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