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NIBR189

产品编号:4086892
规格:≥98% (HPLC)
CAS NO:1599432-08-2
包装规格:5 MG,25 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品编号包装单位单价(元)国内现货国外库存询价单
40868925 MG1190
408689225 MG4390
产品别名

1599432-08-2

NIBR189

(2E)-3-(4-Bromophenyl)-1-(4-(4-methoxybenzoyl)-1-piperazinyl)-2-propen-1-one

NIBR 189

(E)-3-(4-Bromophenyl)-1-(4-(4-methoxybenzoyl)piperazin-1-yl)prop-2-en-1-one

基本信息
Empirical Formula【经验(实验)分子式】
C21H21BrN2O3
Molecular weight
429.31
Biochem/physiol Actions【生化/生理作用】
NBIR189 is a high-affinity, potent and selective EBI2 (GPR183) antagonist (IC50 = 16 nM against 10 nM 7α,25-OHC for binding human EBI2) that inhibits 7α,25-OHC-induced GTPγS binding (IC50 = 8.5 and 7.0 nM, respectively, against 0.33 and 0.1 nM OHC; human EBI2-expressing CHO membrane), calcium mobilization (IC50 = 11 and 15 nM using human or mouse EBI2-transfected cells, respectively), and chemotaxis (IC50 = 0.3 nM against 20 nM OHC-induced U937 migration). NBIR189 displays no inhibitory potency against 5HT2A, muscarinic acetylcholine receptor M2, adrenoreceptor α1A, nor significant affintiy toward 18 other GPCRs/transporters/enzymes, and exhibits good pharmacokinetic properties and oral availability in mice (AUC = 3608 nmol h/L, Cmax = 835 nM, tmax = 1 h, F = 49%; 3 mg/kg p.o.). A useful tool for probing EBI2-mediated physiological functions and autoimmune disorders.
产品性质
Assay【测定】
≥98% (HPLC)
form【形式】
powder
color【颜色】
white to beige
solubility【溶解性】
DMSO: 10 mg/mL, clear (warmed)
storage temp.【储存温度】
room temp
安全信息
Storage Class Code【储存分类代码】
13 - Non Combustible Solids
WGK
WGK 3
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