P-gp
信号通路图
研究领域
抑制剂选择性比较
P-gp产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8028 |
Tariquidar (XR9576)Tariquidar (XR9576) 是一种有效的，选择性的，非竞争性P-glycoprotein抑制剂，在CHrB30细胞系中Kd为5.1 nM，作用于MDR细胞系逆转耐药性。Phase 3。 |
Effects of LEV alone, or in combination with MDRIs, on the migration of L3 stage H. contortus Kirby (A) and WAL (B) larvae; LEV alone shown with solid lines and closed symbols, IVM plus MDRIs shown as dashed lines and open symbols. The concentration of each MDRI in g/mL is shown as subscript after the MDRI name. Each data point represents mean ± SE, n = 9 (pooled data from three experiments, |
|
| S4202 |
Verapamil (CP-16533-1) HClVerapamil HCl (CP-16533-1)是L-型钙通道抑制剂，是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp) 和 CYP3A4。 |
The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
|
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| S0921 |
WilforineWilforine (WR) 是在wilfordii植株中发现的倍半萜吡啶生物碱，可显著地抑制 P-glycoprotein (P-gp) 的外排活性。 |
||
| S3431 |
Encequidar (HM30181)Encequidar (HM30181, HM30181A) 是一种有效的、选择性的三磷酸腺苷结合盒转运体 P-glycoprotein (P-gp) 的抑制剂。 |
||
| S7772 |
Elacridar (GF120918)Elacridar (GF120918, GW120918, GG918, GW0918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。 |
Impact of 10 μM elacridar on the intracellular accumulation of 10 μM nintedanib in DMS114 and DMS114/NIN cells was analyzed by confocal fluorescence microscopy after 1 h drug exposure. The scale bar indicates 10 μm.
|
|
| S3600 |
Schisandrin B (Sch B)Schisandrin B (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATR和P-gp抑制剂。 |
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| S4746 |
(20S)-Protopanaxadiol20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol)，人参皂苷在肠道的主要代谢物，是人参中的活性成分之一。20(S)-Protopanaxadiol 可在耐多种药物的癌细胞中抑制 P-glycoprotein。 |
||
| S7124 |
SC144SC144是一种具有口服活性的小分子gp130抑制剂，能够诱导gp130(S782)磷酸化和去糖基化、抑制STAT3磷酸化和核转位，并进一步抑制其下游靶基因的表达。 |
Suppression of gp130/STAT3 blocks the protective effect of SPRC against Dox-induced cell apoptosis. Cardiomyocytes were pretreated with/without SC144 before SPRC incubation, followed by Dox (1 μM) stimulation for 24 h. (a) Morphological apoptosis was determined by Hoechst 33258 staining. Scale bars, 50 μm.
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| S9563 |
EvodineEvodine是一种天然产物（源于吴茱萸），在中国药典中被记载作为吴茱萸质量评估的生物标志物。Evodine 也是一种有效的 P-gp 的抑制剂。 |
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| S9145 |
SolamargineSolamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition. |
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| S3235 |
SinapineSinapine 是一种从十字花科物种的种子中分离出来的生物碱，具有抗氧化、抗肿瘤和放射防护的作用。Sinapine 通过下调 P-glycoprotein 来抑制Caco-2细胞的增殖。 |
||
| S1481 |
Zosuquidar (LY335979) 3HClZosuquidar 3HCl (LY335979, RS 33295-198, D06387) 是一种有效的P-glycoprotein介导的多药耐抗性的调节剂，无细胞试验中Ki为60 nM。Phase 3。 |
Inhibition of doxorubicin compartmentalization by combined treatment with inhibitors of Abcb1 and Abcc1. A: The cells had been incubated with vehicle or 1 uM zosuquidar plus 15 uM MK571 (ZO/MK), before addition of 1 uM doxorubicin (Doxo) and further cultivation in serum-free medium for 16 h. Shown are typical images of doxorubicin (red) and Hoechst 33342 (blue) fluorescence in Sgpl1+/+ - and Sgpl1-/- -MEFs after treatment as indicated. Two images of Sgpl1-/- -cells treated with doxorubicin plus ZO/MK were selected to show the range of the cellular response. B: Hoechst 33342 staining in MEFs that had been incubated with ZO/MK in the absence of doxorubicin.
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| S9201 |
Levistilide ALevistilide A (Diligustilide), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer. |
||
| S4662 |
AtazanavirAtazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂，常与其他抗HIV药物结合，用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂，也是 P-glycoprotein 的抑制剂和诱导剂。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8028 |
Tariquidar (XR9576)Tariquidar (XR9576) 是一种有效的，选择性的，非竞争性P-glycoprotein抑制剂，在CHrB30细胞系中Kd为5.1 nM，作用于MDR细胞系逆转耐药性。Phase 3。 |
Effects of LEV alone, or in combination with MDRIs, on the migration of L3 stage H. contortus Kirby (A) and WAL (B) larvae; LEV alone shown with solid lines and closed symbols, IVM plus MDRIs shown as dashed lines and open symbols. The concentration of each MDRI in g/mL is shown as subscript after the MDRI name. Each data point represents mean ± SE, n = 9 (pooled data from three experiments, |
|
| S4202 |
Verapamil (CP-16533-1) HClVerapamil HCl (CP-16533-1)是L-型钙通道抑制剂，是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp) 和 CYP3A4。 |
The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
|
|
| S0921 |
WilforineWilforine (WR) 是在wilfordii植株中发现的倍半萜吡啶生物碱，可显著地抑制 P-glycoprotein (P-gp) 的外排活性。 |
||
| S3431 |
Encequidar (HM30181)Encequidar (HM30181, HM30181A) 是一种有效的、选择性的三磷酸腺苷结合盒转运体 P-glycoprotein (P-gp) 的抑制剂。 |
||
| S7772 |
Elacridar (GF120918)Elacridar (GF120918, GW120918, GG918, GW0918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。 |
Impact of 10 μM elacridar on the intracellular accumulation of 10 μM nintedanib in DMS114 and DMS114/NIN cells was analyzed by confocal fluorescence microscopy after 1 h drug exposure. The scale bar indicates 10 μm.
|
|
| S3600 |
Schisandrin B (Sch B)Schisandrin B (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATR和P-gp抑制剂。 |
||
| S4746 |
(20S)-Protopanaxadiol20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol)，人参皂苷在肠道的主要代谢物，是人参中的活性成分之一。20(S)-Protopanaxadiol 可在耐多种药物的癌细胞中抑制 P-glycoprotein。 |
||
| S7124 |
SC144SC144是一种具有口服活性的小分子gp130抑制剂，能够诱导gp130(S782)磷酸化和去糖基化、抑制STAT3磷酸化和核转位，并进一步抑制其下游靶基因的表达。 |
Suppression of gp130/STAT3 blocks the protective effect of SPRC against Dox-induced cell apoptosis. Cardiomyocytes were pretreated with/without SC144 before SPRC incubation, followed by Dox (1 μM) stimulation for 24 h. (a) Morphological apoptosis was determined by Hoechst 33258 staining. Scale bars, 50 μm.
|
|
| S9563 |
EvodineEvodine是一种天然产物（源于吴茱萸），在中国药典中被记载作为吴茱萸质量评估的生物标志物。Evodine 也是一种有效的 P-gp 的抑制剂。 |
||
| S9145 |
SolamargineSolamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition. |
||
| S3235 |
SinapineSinapine 是一种从十字花科物种的种子中分离出来的生物碱，具有抗氧化、抗肿瘤和放射防护的作用。Sinapine 通过下调 P-glycoprotein 来抑制Caco-2细胞的增殖。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1481 |
Zosuquidar (LY335979) 3HClZosuquidar 3HCl (LY335979, RS 33295-198, D06387) 是一种有效的P-glycoprotein介导的多药耐抗性的调节剂，无细胞试验中Ki为60 nM。Phase 3。 |
Inhibition of doxorubicin compartmentalization by combined treatment with inhibitors of Abcb1 and Abcc1. A: The cells had been incubated with vehicle or 1 uM zosuquidar plus 15 uM MK571 (ZO/MK), before addition of 1 uM doxorubicin (Doxo) and further cultivation in serum-free medium for 16 h. Shown are typical images of doxorubicin (red) and Hoechst 33342 (blue) fluorescence in Sgpl1+/+ - and Sgpl1-/- -MEFs after treatment as indicated. Two images of Sgpl1-/- -cells treated with doxorubicin plus ZO/MK were selected to show the range of the cellular response. B: Hoechst 33342 staining in MEFs that had been incubated with ZO/MK in the absence of doxorubicin.
|
|
| S9201 |
Levistilide ALevistilide A (Diligustilide), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer. |
||
| S4662 |
AtazanavirAtazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂，常与其他抗HIV药物结合，用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂，也是 P-glycoprotein 的抑制剂和诱导剂。 |
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