产品说明
应用
NIBR-0213 may be used as a selective sphingosine-1-phosphate receptor 1 (S1P1) antagonist to assess S1P-mediated nuclear factor kappa B (NF-κB)-p65 nuclear translocation in human induced astrocytes.
生化/生理作用
NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist that blocks S1P1-selective ligand AUY954-induced Ca2+ mobilization (IC50 = 2.5 nM using human S1P1-transfected HeLa cells; IC50 >10 μM with human S1P2, S1P3, or S1P4 transfectants) and S1P-induced GTPγS recruitment (IC50 = 2.0/2.3/8.5 nM using membrane from human/murine/rat S1P1-transfected CHO cells; IC50 >10 μM with membrane from human S1P5 transfectant). NIBR-0213 induces long-lasting peripheral blood lymphocyte reduction in rats (EDmax = 1 mg/kg, ED50 = 0.2 mg/kg; p.o.) and exhibits therapeutic efficacy (30 mg/kg p.o; BID) in experimental autoimmune encephalomyelitis (EAE), a murine model of multiple sclerosis (MS), with no adverse effects to the animals.
基本信息
| 经验(实验)分子式 | C27H29ClN2O3 |
| 分子量 | 464.98 |
| MDL编号 | MFCD25977008 |
产品性质
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | −20℃ |
| SMILES string | C[C@@H](C(O)=O)NC(C1=C(C)C=C(C2=CC=CC(N[C@@H](C3=CC=C(Cl)C(C)=C3)C)=C2)C=C1C)=O |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
