2. Membrane Transporter/Ion Channel
  3. BCRP
  4. P-gp/BCRP-IN-1

P-gp/BCRP-IN-1 (compound 19) 是一种潜在的、相对安全的、口服有效的外排转运蛋白(P-gp 和 BCRP) 抑制剂。P-gp/BCRP-IN-1 通过抑制 P-gp 和 BCRP 的外排功能产生耐药性逆转，P-gp/BCRP-IN-1可克服紫杉醇的耐药性，提高紫杉醇的口服生物利用度。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

P-gp/BCRP-IN-1 Chemical Structure

P-gp/BCRP-IN-1 Chemical Structure

CAS No. : 2764596-06-5

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

P-gp/BCRP-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel)[1].

IC50 & Target

P-gp

 

体外研究
(In Vitro)

P-gp/BCRP-IN-1 (compound 19) (0-200 μM, 48 h) has a weak anti-proliferative activity against A549 cells, and shows low cytotoxicity to the K562 , K562/A02, MDCK-II, MDCK-II-BCRP cells[1].
P-gp/BCRP-IN-1 (48 h) exhibits the great reversal effect of resistance to both ADM (Adriamycin) and MX (Mitoxantrone) in K562/A02 cells and MDCK-II-BCRP cells, and increases the reversal activity of ADM (0-5 μM) and MX (0-20 μM) in a concentration-dependent manner[1].
P-gp/BCRP-IN-1 (0-5 μM, 4 h) increases drug accumulation and prevents efflux of P-gp and BCRP[1].
P-gp/BCRP-IN-1 (0-5 μM, 48 h) dose not affect the expression of P-gp as well as BCRP protein[1].
P-gp/BCRP-IN-1 (0-200 μM, 4 h) decreases the viability of Caco-2 cells, inhibits the intestinal P-gp-mediated efflux of PTX and increases its concentration in the intestinal cells, can enhance the absorption and bioavailability[1].
P-gp/BCRP-IN-1 prevents intracellular accumulation of anti-neoplastic drugs by impairing the function of P-gp and BCRP[1].

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

P-gp/BCRP-IN-1 相关抗体:

Cell Proliferation Assay

Cell Line: A549 cells, chemo-sensitive cell lines (K562, MDCK-II), chemo-resistant cell lines (K562/A02, MDCK-II-BCRP)[1]
Concentration: 200, 100, 50, 25, 12.5, 6.25, 3.125, 1.56 and 0 μM
Incubation Time: 24, 48 h
Result: Had a weak anti-proliferative activity against A549 cells, with an IC50 of 46.28 μM, and showed low cytotoxicity to the K562 , K562/A02, MDCK-II, MDCK-II-BCRP cells, with IC50 values of 72.81, 43.29, 87.69, 81.22 μM, respectively.

Cell Viability Assay

Cell Line: K562/A02 cells and MDCK-II-BCRP cells[1]
Concentration: 5 μM
Incubation Time: 48 h
Result: Increased the reversal activity of ADM (0-5 μM) and MX (0-20 μM) in a concentration-dependent manner, exhibited the great reversal effect of resistance to both ADM and MX in K562/A02 cells and MDCK-II-BCRP cells, with IC50 values (at 5 μM) of 2.41 and 18.43 μM, RF (reversal fold, at 5 μM) of 40.51 and 37.40, and EC50of 65.31 and 98.22 nM, respectively.

Western Blot Analysis

Cell Line: K562/A02 cells and MDCK-II-BCRP cells, K562 and MDCK-II cells.[1]
Concentration: 0, 0.5, 1, 5 μM
Incubation Time: 48 h
Result: Did not affect the expression of P-gp as well as BCRP protein, exerted resistance reversal without affecting the expression of P-gp as well as BCRP protein, but probably by inhibiting the efflux function of P-gp and BCRP.

Cell Viability Assay

Cell Line: Caco-2 cells[1]
Concentration: 1.25, 5, 10, 20, 30, 50, 100, 200 μM
Incubation Time: 4 h
Result: Decreased the viability of Caco-2 cells to less than 20% at concentrations of 30 and 50 μM respectively, significantly decreased the Papp (apparent permeability coefficient) value, inhibited the intestinal P-gp-mediated efflux of PTX and increased its concentration in the intestinal cells, which could eventually enhance the absorption and bioavailability of the orally administered drug.
体内研究
(In Vivo)

P-gp/BCRP-IN-1 (compound 19) (Male SD rats; 5 mg/kg PTX (IV), 20 mg/kg PTX (PO), 20 mg/kg PTX and 10 mg/kg compound 19 (PO); once) increases the bioavailability of PTX when PTX is given orally[1].
Pharmacokinetic Parameters of P-gp/BCRP-IN-1 in male SD rats[1].

PTX (5 mg/kg) PTX (20 mg/kg) PTX (20 mg/kg) with 19 (10 mg/kg)
Routemax (h) IV PO PO
AUC0-t (ng*h/mL) 1734.95 ± 244.28 610.89 ± 45.62 3131.51 ± 63.17
Cmax (ng/mL) 925.86 ± 31.39 112.09 ± 25.46 652.31 ± 41.93
Tmax (h) 0.44 ± 0.05 2.00 ± 0.03 2.51 ± 0.19
T1/2 (h) 0.12 ± 0.03 1.35 ± 0.05 1.68 ± 0.15
Vd/F (L) 5.06 ± 0.09 67.38 ± 12.54 16.04 ± 0.08
CL/F (L/h) 2.88 ± 0.14 32.74 ± 5.42 6.18 ± 0.36
F (%) 100 8.80 45.1

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

Animal Model: Male SD rats (n = 15, three groups)[1]
Dosage: 5 mg/kg PTX (IV); 20 mg/kg PTX (PO); 20 mg/kg PTX with 10 mg/kg compound 19 (PO)
Administration: IV, PO, once (Pharmacokinetic Analysis)
Result: Increased the bioavailability of PTX when PTX was given orally.
分子量

488.97

Formula

C27H25ClN4O3
CAS 号
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.
纯度 & 产品资料
参考文献

P-gp/BCRP-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

P-gp/BCRP-IN-12764596-06-5BCRPBreast cancer resistance proteinABCG2Efflux transporterMultidrug resistance (MDR)Paclitaxel (PTX)Oral bioavailabilityLow cytotoxicityOrally activeInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
P-gp/BCRP-IN-1
目录号：
HY-144393
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z