货号	规格	价格	上海	北京	珠海	重庆	武汉
S89378-5mg买3赠1	99.80%	￥900.00 S89378-5mg ￥900.00 现货（买3赠1）	9 9	-	-	-	-
S89378-10mg买3赠1	99.80%	￥1300.00 S89378-10mg ￥1300.00 现货（买3赠1）	5 5	-	-	-	-
S89378-25mg	≥98%	￥2600.00 S89378-25mg ￥2600.00 3-5天	0 货期：3-5天	-	-	-	-
S89378-100mg	≥98%	￥5920.00 S89378-100mg ￥5920.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ35S assays

靶点：

LPL Receptor;LPLReceptor

体外研究：

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 Ca2+ 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 GTPγ35S 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 GTPγ35S assay. NIBR-0213 is a competitive S1P1 antagonist with a calculated Kd of 0.37±0.031 nM.

体内研究：

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. Animal Model: Lewis or Wistar rats (220-250 g, males) Dosage: 30 mg/kg Administration: Orally Result: Reduced the PBL counts by 75%-85% within 14 hr and maintained this effect up to 24 hr posttreatment. Animal Model: C57BL/6 mice bearing EAE model Dosage: 30 mg/kg and 60 mg/kg Administration: 30 mg/kg twice per day (BID) for 3 days and then increased to 60 mg/kg BID until the remainder of the experiment. In total, the treatment lasted 26 days Result: Resulted in a gradual reduction in disease-scores, with a divergence from vehicle controls that became significant after 5 days.

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

备注：

1: Bigaud M, Dincer Z, Bollbuck B, Dawson J, Beckmann N, Beerli C, Fishli-Cavelti G, Nahler M, Angst D, Janser P, Otto H, Rosner E, Hersperger R, Bruns C, Quancard J. Pathophysiological Consequences of a Break in S1P1-Dependent Homeostasis of Vascular Permeability Revealed by S1P1 Competitive Antagonism. PLoS One. 2016 Dec 22;11(12):e0168252. doi: 10.1371/journal.pone.0168252. eCollection 2016. PubMed PMID: 28005953; PubMed Central PMCID: PMC5179015.

2: Quancard J, Bollbuck B, Janser P, Angst D, Bers

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.151 ml	10.753 ml	21.506 ml
5 mM	0.43 ml	2.151 ml	4.301 ml
10 mM	0.215 ml	1.075 ml	2.151 ml
50 mM	0.043 ml	0.215 ml	0.43 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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计算重置

NIBR0213

(2S)-2-[[4-[3-[[(1R)-1-(4-chloro-3-methylphenyl)ethyl]amino]phenyl]-2,6-dimethylbenzoyl]amino]propanoic acid

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)