1. Anti-infection GPCR/G Protein
  2. EBV EBI2/GPR183
  3. NIBR189

NIBR189 是 EBI2 (Epstein-Barr virus-induced gene 2) 的拮抗剂。NIBR189 抑制人和老鼠的 EBI2, IC50 值分别为 11 和 16 nM。NIBR189 可用于自身免疫病的研究。

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NIBR189 Chemical Structure

NIBR189 Chemical Structure

CAS No. : 1599432-08-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1155
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1 mg ¥477
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5 mg ¥1050
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10 mg ¥1800
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50 mg ¥5800
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NIBR189 is an EBI2 (Epstein-Barr virus-induced gene 2) antagonist. NIBR189 inhibits human and mouse EBI2 with IC50s of 11 and 16 nM, respectively. NIBR189 can be used for the research of autoimmune diseases[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
11 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
[PMID: 24678947]
CHO IC50
15 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
[PMID: 24678947]
CHO IC50
7 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
[PMID: 24678947]
CHO IC50
8.5 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
[PMID: 24678947]
U-937 IC50
0.3 nM
Compound: 4m, NIBR189
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
[PMID: 24678947]
U-937 IC50
9 nM
Compound: 4m, NIBR189
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
[PMID: 24678947]
体外研究
(In Vitro)

NIBR189 (0-1 μM; 3 h) blocks migration of U937 cells[1].
NIBR189 (0-10 μM) blocks oxysterol-dependent activation with an IC50 value of 9 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay [1]

Cell Line: U937 cell lines
Concentration: 0-1 μM
Incubation Time: 3 hours
Result: Blocked the direct migration of U937 cells with an IC50 value of 0.3 nM.
体内研究
(In Vivo)

1.19 Pharmacokinetic Properties of NIBR189 in Mice[1].

Mice
IV 1 mg/kg
Mice
PO 3 mg/kg
CL (μL/min/mg) 16
t1/2 (h) 1.1
Vss (L/kg) 1.4
AUC (nmol·h/L) 2435 3608
Cmax (nmol/L) 835
tmax (h) 1
F (%) 49

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

429.31

Formula

C21H21BrN2O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (116.47 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3293 mL 11.6466 mL 23.2932 mL
5 mM 0.4659 mL 2.3293 mL 4.6586 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.82 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3293 mL 11.6466 mL 23.2932 mL 58.2330 mL
5 mM 0.4659 mL 2.3293 mL 4.6586 mL 11.6466 mL
10 mM 0.2329 mL 1.1647 mL 2.3293 mL 5.8233 mL
15 mM 0.1553 mL 0.7764 mL 1.5529 mL 3.8822 mL
20 mM 0.1165 mL 0.5823 mL 1.1647 mL 2.9116 mL
25 mM 0.0932 mL 0.4659 mL 0.9317 mL 2.3293 mL
30 mM 0.0776 mL 0.3882 mL 0.7764 mL 1.9411 mL
40 mM 0.0582 mL 0.2912 mL 0.5823 mL 1.4558 mL
50 mM 0.0466 mL 0.2329 mL 0.4659 mL 1.1647 mL
60 mM 0.0388 mL 0.1941 mL 0.3882 mL 0.9705 mL
80 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.7279 mL
100 mM 0.0233 mL 0.1165 mL 0.2329 mL 0.5823 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NIBR189
目录号:
HY-12336
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