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描述 | NIBR-0213 emerges as a potent, orally active antagonist of the S1P1 receptor, demonstrating efficacy in experimental autoimmune encephalomyelitis (EAE), a model of multiple sclerosis. NIBR-0213 exhibits remarkable potency and selectivity towards S1P1 across species, with IC50 values of 2.0 nM and 2.3 nM in human and rat S1P1 receptors, respectively, in GTPγ35S assays[1]. |
Animal study | In therapeutic models, NIBR-0213 demonstrates significant biological effects. When administered orally at 30 mg/kg to rats, it dramatically reduces peripheral blood lymphocyte (PBL) counts by 75%-85% within 14 hours, maintaining this suppression up to 24 hours post-treatment. This effect suggests a strong immunomodulatory capability, which is critical for diseases where lymphocyte migration and activation play pivotal roles[1].Moreover, the efficacy of NIBR-0213 extends to disease models, as doses of 30 mg/kg and 60 mg/kg have been effective in a mouse model of experimental autoimmune encephalomyelitis (EAE), a standard model for studying multiple sclerosis. This outcome suggests its potential for therapeutic application in autoimmune diseases, particularly for conditions that mimic the pathophysiology of multiple sclerosis[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.15mL 0.43mL 0.22mL |
10.75mL 2.15mL 1.08mL |
21.51mL 4.30mL 2.15mL |
CAS号 | 1233332-14-3 |
分子式 | C27H29ClN2O3 |
分子量 | 464.98 |
SMILES Code | C[C@H](NC(C1=C(C)C=C(C2=CC=CC(N[C@@H](C3=CC=C(Cl)C(C)=C3)C)=C2)C=C1C)=O)C(O)=O |
MDL No. | MFCD25977008 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, store in freezer, under -20°C |