您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Ozanimod(RPC1063)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Ozanimod(RPC1063)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ozanimod(RPC1063)图片
CAS NO:1306760-87-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)404.46
FormulaC23H24N4O3
CAS No.1306760-87-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 81 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (24.7 mM)
Other info

Chemical Name: (S)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1H-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile

InChi Key: XRVDGNKRPOAQTN-FQEVSTJZSA-N

InChi Code: InChI=1S/C23H24N4O3/c1-14(2)29-21-9-6-15(12-16(21)13-24)23-26-22(27-30-23)19-5-3-4-18-17(19)7-8-20(18)25-10-11-28/h3-6,9,12,14,20,25,28H,7-8,10-11H2,1-2H3/t20-/m0/s1

SMILES Code: N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[C@@H]4NCCO)=NO2)=CC=C1OC(C)C

SynonymsRPC1063; RPC-1063; RPC 1063
实验参考方法
In Vitro

In vitro activity: In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation.


Kinase Assay: Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 nM in [35S]-GTPγS binding, respectively.


Cell Assay: Ozanimod(RPC1063) was a specific agonist for S1P1 and S1P5 receptors. The EC50values were 160 ± 60 pM and 410 ± 160 pM for S1P1 receptors in the inhibition of cAMP generation and[35S]-GTPγS binding. The 83% Emax value of ozanimod against S1P5 receptor was 11 ± 4.3 nM. RPC1063 dose-dependently decreased S1P1 receptor re-expression on the cell surface and resulted in near complete and sustained loss of cell surface receptor expression at concentrations above 10 nM in S1P1 receptor-HEK293T cells after 1 h incubation.

In VivoIn vivo, Ozanimod shows high oral bioavailability and volume of distribution. In a MOG-induced EAE mouse model, Ozanimod (3 mg/kg, p.o.) suppresses clinical symptoms. In a rat TNBS model of inflammatory bowel disease, Ozanimod (1.2 mg/kg, p.o.) inhibits clinical and histological disease scores. In a Naive CD4+CD45Rbhi T cell adoptive transfer model, Ozanimod (1.2 mg/kg, p.o.) also significantly reduced disease severity as assessed by measuring the degree of inflammation, gland loss, hyperplasia, neutrophil infiltrate and mucosal thickness.
Animal modelMOG-induced EAE model in C57Bl6 mice, TNBS model of inflammatory bowel disease in male Sprague Dawley rats, and Naive CD4+CD45Rbhi T cell adoptive transfer model in SCID mice
Formulation & DosageDissolved in 5% DMSO, 5% Tween-20, 90% 0.1N HCl; 0.1-3 mg/kg; oral givage
References

Br J Pharmacol. 2016 Jun;173(11):1778-92