1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. P-gp inhibitor 21

P-gp inhibitor 21 (Compound 56) 是一种 P-糖蛋白 (P-gp) 转运抑制剂,可以逆转 P-gp 介导的多药耐药性 (MDR),并在小鼠模型中表现出抗肿瘤功效,无显著细胞毒性。

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Custom Peptide Synthesis

P-gp inhibitor 21 Chemical Structure

P-gp inhibitor 21 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity[1].

体外研究
(In Vitro)

P-gp inhibitor 21 抑制细胞 KBV200 和 NCI/ADR-RES (与 VNR 共同作用) 的增殖,IC50 分别为 2.4 和 27.9 nM[ 1]

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

体内研究
(In Vivo)

P-gp inhibitor 21 (75 mg/kg,腹腔注射) KBV200 异种移植 BALB/c 裸鼠中的肿瘤生长并恢复 MDR 肿瘤对 VNR 的敏感性,且无明显毒性[1]

P-gp inhibitor 21 在小鼠模型中的药代动力学分析[1]

route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (ng·h/mL) AUCinf_obs (ng·h/mL) CLobs (mL/min/kg) MRTinf_obs (h) Vss (mL/kg) F (%)
iv 1 - - 1260 1263 33.5 0.75 1528 -
po 30 0.25 34.4 32.3 43.4 - 3.11 - 0.09

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

Animal Model: KBV200 xenograft BALB/c nude mice[1]
Dosage: 75 mg/kg
Administration: i.p.
Result: Suppressed tumor growth without significant body weight loss.
分子量

458.63

Formula

C27H42N2O4

Unlabeled Cas

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
  • 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.

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产品名称:
P-gp inhibitor 21
目录号:
HY-162396
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