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

CAS No. :

MCE 站：P-gp/BCRP-IN-1

产品活性：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。

研究领域：Membrane Transporter/Ion Channel

作用靶点：BCRP

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.
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.
P-gp/BCRP-IN-1 (0-5 μM, 4 h) increases drug accumulation ａnd prevents efflux of P-gp ａnd BCRP.
P-gp/BCRP-IN-1 (0-5 μM, 48 h) dose not affect the expression of P-gp as well as BCRP protein.
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.
P-gp/BCRP-IN-1 prevents intracellular accumulation of anti-neoplastic drugs by impairing the function of P-gp ａnd BCRP.

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.
Pharmacokinetic Parameters of P-gp/BCRP-IN-1 in male SD rats.

相关产品：Ko 143  |  Elacridar  |  CP-100356 hydrochloride  |  Fumitremorgin C  |  Zamicastat  |  KS176  |  PCI 29732  |  (S)-ML753286  |  YHO-13177  |  ML230  |  YHO-13351 free base  |  6,8-Diprenylnaringenin  |  Ac32Az19  |  FD 12-9  |  PD166326  |  Triclabendazole sulfoxide  |  Triclabendazole sulfoxide-13C,d3  |  Triclabendazole sulfoxide-d3  |  UR-MB108

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物  |  寡核苷酸

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。