NIBR0213
目录号: PL06757
CAS No. :1233332-14-3
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中文名称
NIBR0213
中文别名
(S)-2-({3'-[(R)-1-(4-Chloro-3-methyl-phenyl)-ethylamino]-3,5-dimethyl-biphenyl-4-carbonyl}-amino)-propionic acid
英文名称
NIBR0213
英文别名
(S)-2-({3′-[(R)-1-(4-Chloro-3-methyl-phenyl)-ethylamino]-3,5-dimethyl-biphenyl-4-carbonyl}-amino)-propionic acid;N-[[3′-[[(1R)-1-(4-Chloro-3-methylphenyl)ethyl]amino]-3,5-dimethyl[1,1′-biphenyl]-4-yl]carbonyl]-L-alanine;NIBR 0213;NIBR0213;(2S)-2-[[4-[3-[[(1R)-1-(4-chloro-3-methylphenyl)ethyl]amino]phenyl]-2,6-dimethylbenzoyl]amino]propanoic acid;N-[[3'-[[(1R)-1-(4-chloro-3-methylphenyl)ethyl]amino]-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]-L-alanine;GTPL6997;BDBM50494303;Q27087922
Cas No.
1233332-14-3
分子式
C27H29ClN2O3
分子量
464.98
包装储存
Please store the product under the recommended conditions in the Certificate of Analysis.
产品详情
NIBR-0213 是一种有效的选择性 S1P1 拮抗剂,对实验性自身免疫性脑脊髓炎有效。在 GTPγ35S 试验中,NIBR-0213 有效作用于人和大鼠 S1P1,IC50 分别为 2.0 nM 和 2.3 nM。
生物活性
NIBR-0213 is a potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC 50  of 2.0 nM and 2.3 nM, respectively) in GTPγS assays.
体外研究(In Vitro)
NIBR-0213 displays an inhibitory activity on hS1P1 with an IC50 of 2.5 nM whereas it is inactive (IC50 >10 μM) on S1P2, S1P3, and S1P4 in Ca mobilization assays.
NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγS assays, whereas on mouse S1P1 with an IC50 of 8.5 nM.
NIBR-0213 shows an ~3,000-fold selectivity against human S1P5 in the GTPγS assay.
NIBR-0213 is a competitive S1P1 antagonist with a calculated Kd of 0.37±0.031 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
NIBR-0213 (given orally at 30 mg/kg to rats) reduces the peripheral blood lymphocyte (PBL) counts by 75%-85% within 14 hr and maintained this effect up to 24 hr posttreatment.
NIBR-0213 (30 mg/kg and 60 mg/kg) is efficacious when given therapeutically in a mouse experimental autoimmune encephalomyelitis (EAE) model.
The PK properties of NIBR-0213 shows a moderate clearance (26 mL/min/kg) and a high oral bioavailability (69%), leading to significant exposure after oral dosing. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
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.
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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