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NIBR0213 {[allProObj[0].p_purity_real_show]}

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NIBR0213是一种高效且具有口服活性的选择性S1P1受体拮抗剂,对实验性自身免疫性脑脊髓炎(EAE)具有显著疗效。在GTPγ35S试验中,NIBR-0213 对人类和大鼠S1P1的IC50分别为2.0 nM和2.3 nM,展示了对S1P1受体的强效拮抗作用。该化合物可用于研究自身免疫性疾病。

NIBR0213 化学结构 CAS号:1233332-14-3
NIBR0213 化学结构
CAS号:1233332-14-3
NIBR0213 3D分子结构
CAS号:1233332-14-3
NIBR0213 化学结构 CAS号:1233332-14-3
NIBR0213 3D分子结构 CAS号:1233332-14-3
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NIBR0213 纯度/质量文件 产品仅供科研

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NIBR0213 生物活性

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].
体内研究

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].

体外研究

NIBR-0213 showcases targeted inhibitory activity on the hS1P1 receptor with a notably low IC50 of 2.5 nM, indicating its high potency. Its effectiveness is highly specific, as it does not significantly inhibit S1P2, S1P3, and S1P4 receptors in calcium mobilization assays, where the IC50 values exceed 10 μM, underscoring its selective action[1].

NIBR-0213's potency is consistent across species, displaying IC50 values of 2.0 nM for human S1P1 and 2.3 nM for rat S1P1 in GTPγ35S assays. This potency slightly decreases in mouse S1P1 with an IC50 of 8.5 nM, but it remains highly effective. Additionally, NIBR-0213 exhibits approximately 3,000-fold selectivity against the human S1P5 receptor in the same assay, reinforcing its selectivity towards S1P1[1].

As a competitive antagonist of S1P1, NIBR-0213's affinity for the receptor is further quantified by a calculated Kd of 0.37 ± 0.031 nM, which is indicative of its strong binding efficiency and potential for high efficacy in vivo[1].

NIBR0213 参考文献

[1]Jean Quancard, et al. A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis. Chem Biol. 2012 Sep 21;19(9):1142-51.

NIBR0213 实验方案

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

NIBR0213 技术信息

CAS号1233332-14-3
分子式C27H29ClN2O3
分子量 464.984
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度
动物实验配方
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