2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Anti-infection Metabolic Enzyme/Protease
  3. Glucocorticoid Receptor Cytochrome P450 HCV Protease
  4. BI 653048

BI 653048 是一种选择性且口服的非甾体类糖皮质激素 (glucocorticoid (GC)) 激动剂，其 IC50 值为 55 nM。BI 653048 抑制 CP1A2，CYP2D6，CYP2C9，CYP2C19 和 CYP3A4 的活性并降低对 hERG 离子通道的亲和力 (IC50>30 μM)。BI 653048 源于专利 WO2005028501A1 (化合物 103)，它也是一种 HCV NS3 protease 抑制剂，可以减少感染丙型肝炎病毒的病毒载量。

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BI 653048 Chemical Structure

BI 653048 Chemical Structure

CAS No. : 1198784-72-3

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规格 价格 是否有货 数量
1 mg ￥4500
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Customer Review

Other Forms of BI 653048:

BI 653048 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM[1]. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM)[2]. BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus[3].

IC50 & Target[2]

CYP1A2

50 μM (IC50)

CYP2D6

41 μM (IC50)

CYP2C9

12 μM (IC50)

CYP2C19

9 μM (IC50)

CYP3A4

8 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 30 μM
Compound: (R)-39
Inhibition of human ERG channel expressed in recombinant HEK293 cells by whole cell patch-clamp technique
Inhibition of human ERG channel expressed in recombinant HEK293 cells by whole cell patch-clamp technique
[PMID: 25516791]
体外研究
(In Vitro)

BI 653048 exhibits an improved drug-like properties, inhibits CP1A2 ,CYP2D6 ,CYP2C9, CYP2C19 and CYP3A4 with IC50 values of 50 µM, 41 µM, 12 µM, 9 µM,and 8 µM, respectively[2].
BI 653048 reduces affinity for the hERG ion channel with an IC50>30 μM in recombinant HEK293 cells expressing the human ERG potassium channel[2].
BI 653048 inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50 value of 100 nM[2].

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

BI 653048 相关抗体:
体内研究
(In Vivo)

BI 653048 (oral administration; 3, 10, and 30 mg/kg) at 3 mg/kg has nonsignificant decreases for all measured histology parameters (ankle inflammation, pannus formation, cartilage damage, and bone resorption), Mid-dose (10 mg/kg) treatment significantly decreases pannus and bone resorption (33%) as well as summed scores (27%), while at high dose (30 mg/kg), all parameters are significantly decreased (87–96%). The ED50 value for the summed scores is 14 mg/kg[2].

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

Animal Model: Mice[2]
Dosage: 3, 10, and 30 mg/kg
Administration: Oral administration
Result: Exhibits significant decreases for all measured histology parameters at high doses.
Clinical Trial
分子量

515.52

Formula

C23H25F4N3O4S
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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (193.98 mM; 超声助溶; 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 1.9398 mL 9.6989 mL 19.3979 mL
5 mM 0.3880 mL 1.9398 mL 3.8796 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 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

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

BI 653048 相关分类

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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9398 mL 9.6989 mL 19.3979 mL 48.4947 mL
5 mM 0.3880 mL 1.9398 mL 3.8796 mL 9.6989 mL
10 mM 0.1940 mL 0.9699 mL 1.9398 mL 4.8495 mL
15 mM 0.1293 mL 0.6466 mL 1.2932 mL 3.2330 mL
20 mM 0.0970 mL 0.4849 mL 0.9699 mL 2.4247 mL
25 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9398 mL
30 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6165 mL
40 mM 0.0485 mL 0.2425 mL 0.4849 mL 1.2124 mL
50 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
60 mM 0.0323 mL 0.1616 mL 0.3233 mL 0.8082 mL
80 mM 0.0242 mL 0.1212 mL 0.2425 mL 0.6062 mL
100 mM 0.0194 mL 0.0970 mL 0.1940 mL 0.4849 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.

Keywords:

BI 6530481198784-72-3BI653048BI-653048Glucocorticoid ReceptorCytochrome P450HCV ProteaseCYPsHCVNS3proteaseInhibitorinhibitorinhibit

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目录号：
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