33
20
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T28396 |
PGP-4008
PGP 4008,PGP4008 |
P-gp | Membrane transporter/Ion channel; Neuroscience |
PGP-4008 是一种具有选择性和有效性的 P-糖蛋白 (Pgp) 抑制剂,通过与Doxorubicin联合给药来抑制肿瘤生长。 | |||
T16466 |
Penicillin G Procaine
PGP |
Others | Others |
Penicillin G Procaine is a β-lactam antibiotic and is a crystalline complex produced by chemically combining penicillin G with procaine. | |||
T12341 |
P-gp inhibitor 1
|
Others; P-gp | Membrane transporter/Ion channel; Neuroscience; Others |
P-gp inhibitor 1 抑制逆转 P-糖蛋白介导的多药耐药性,EC50 为 57.9 nM(K562/A02 细胞)。 | |||
T11071 |
Dofequidar fumarate
MS-209 |
P-gp | Membrane transporter/Ion channel; Neuroscience |
Dofequidar fumarate (MS-209) 是口服活性的喹啉化合物,通过抑制 ABCB1/P-gp 和 ABCC1/MDR 相关蛋白 1 来克服 MDR。 | |||
T6287 |
Tariquidar
XR9576,他立喹达 |
P-gp | Membrane transporter/Ion channel; Neuroscience |
Tariquidar (XR9576) 是一种特异性有效的P-糖蛋白抑制剂,Kd 为 5.1 nM。 | |||
T16561 |
Polyoxyethylene stearate
POES,聚氧乙烯硬脂酸酯 |
Antibacterial; P-gp | Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Polyoxyethylene stearate (POES) 是一种非离子乳化剂。 | |||
T8426 |
Encequidar
HM30181,HM30181A |
P-gp | Membrane transporter/Ion channel; Neuroscience |
Encequidar (HM30181A) 是一种选择性 P-糖蛋白抑制剂。 | |||
T4059 |
Selamectin
UK-124114,司拉克丁,塞拉菌素 |
Chloride channel; P-gp; Parasite | Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Selamectin (UK-124114) 是半合成的大环内酯,是一种驱虫剂,可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。它还是抗寄生虫剂,可激活神经元和咽肌中的谷氨酸门控氯离子通道,以预防恶丝虫,淋巴丝虫和线虫感染。它还是 P-糖蛋白底物和抑制剂,IC50为 120 nM。 | |||
T0351 |
Risperidone
Risperidal,R 64 766,利培酮 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; P-gp | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Risperidone (R 64 766) 是5-HT2受体阻断剂、P-糖蛋白抑制剂和多巴胺 D2受体的拮抗剂,对 5-HT2A 和多巴胺 D2受体的 Ki 值分别为 4.8 和 5.9 nM。 | |||
T11578L |
Encequidar mesylate
HM30181 mesylate,HM30181A mesylate |
P-gp | Membrane transporter/Ion channel; Neuroscience |
Encequidar mesylate (HM30181A mesylate) 是竞争性有效的 P-糖蛋白抑制剂。 | |||
T13383 |
Zamicastat
BIA 5-1058 |
BCRP; Hydroxylase; P-gp | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Zamicastat (BIA 5-1058) 是多巴胺 β-羟化酶 (DBH) 抑制剂,可透过血脑屏障引起中枢和周边效应,具有降血压作用。它也是一种浓度依赖性的双重 P-gp 和 BCRP 抑制剂,IC50值分别为 73.8 和 17.0 μM。 | |||
T8389 |
Trifluoperazine
三氟拉嗪,trifluoroperazine |
CaMK; Dopamine Receptor; Influenza Virus; Adrenergic Receptor; P-gp; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Trifluoperazine (trifluoroperazine) 是一种多巴胺 D2 受体抑制剂,可治疗精神分裂症。它是NUPR1抑制剂,具有抗癌活性。它是α1-adrenergic 受体拮抗剂,是流感病毒形态发生的可逆抑制剂。 | |||
T12340 | P-gp modulator 1 | Others | Others |
P-gp modulator 1 is a high affinity and orally available P-glycoprotein (Pgp) modulator | |||
T1634 |
Glibenclamide
格列本脲,Glyburide |
Potassium Channel; Mitochondrial Metabolism; CFTR; P-gp; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Glibenclamide (Glyburide) 是一种具有口服活性的 ATP 敏感的 K+通道抑制剂,可研究糖尿病和肥胖。它抑制 P-糖蛋白,可直接结合并阻断 KATP 的 SUR1亚基并抑制囊性纤维化跨膜传导调节蛋白。它通过诱导膜离子通透性干扰线粒体生物能,可诱导自噬。 | |||
T0100L |
Atazanavir
Zrivada,Reyataz,Latazanavir,阿扎那韦,BMS-232632 |
P450; SARS-CoV; HIV Protease; P-gp | Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome |
Atazanavir (BMS-232632) 是一种高选择性的HIV-1蛋白酶抑制剂,可研究艾滋病毒感染。它也是SARS-CoV 3CLpro 的抑制剂,IC50为 3.49 μM。它是CYP3A4的底物和抑制剂,也是P-糖蛋白的抑制剂和诱导剂。 | |||
T20656 |
Verapamil
NSC 135784,维拉帕米,NSC-135784,CP-16533-1,(±)-Verapamil |
P450; Calcium Channel; P-gp | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Verapamil (CP-16533-1) 是一种钙通道阻滞剂,是一种口服有效的 P-gp 抑制剂。Verapamil 抑制 CYP3A4,可用于治疗高血压、心律失常和心绞痛的研究。 | |||
T16339 |
Norverapamil hydrochloride
(±)-Norverapamil hydrochloride,D591 hydrochloride,盐酸去甲维拉帕米 |
Calcium Channel; P-gp; Drug Metabolite | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Norverapamil hydrochloride (D591 hydrochloride) 是 Verapamil 的 N-去甲基代谢物,是 L 型钙通道阻滞剂和 P-糖蛋白 (P-gp) 功能抑制剂。 | |||
T2657 |
Elacridar
GW0918,依克立达,GW120918,GF120918,GG918 |
BCRP; P-gp | Membrane transporter/Ion channel; Neuroscience |
Elacridar (GG918) 是一种有效的 P-糖蛋白和BCRP 的抑制剂。 | |||
T1010 |
Verapamil hydrochloride
Manidon,盐酸维拉帕米,(±)-Verapamil hydrochlorid,Verapamil HCl,Calcan hydrochloride |
P450; Calcium Channel; P-gp | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Verapamil hydrochloride (Verapamil HCl) 是一种钙通道阻滞剂,是一种可口服的 P 糖蛋白 (P-gp) 抑制剂,可抑制CYP3A4,用于高血压、心律不齐和心绞痛的研究。 | |||
T1222 |
Trifluoperazine dihydrochloride
Trifluoperazine 2HCl,盐酸三氟拉嗪,SKF5019,Urinox |
CaMK; Dopamine Receptor; Influenza Virus; Adrenergic Receptor; P-gp; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Trifluoperazine dihydrochloride (SKF5019) 是一种抗精神病药物,靶向中枢多巴胺受体。它是流感病毒形态发生的可逆抑制剂,是NUPR1抑制剂,具有抗癌活性。它是钙调蛋白抑制剂,还可抑制 P-糖蛋白,可研究精神分裂症。 | |||
T0100 |
Atazanavir sulfate
阿扎那韦硫酸盐,BMS-232632,BMS-232632 sulfate,硫酸阿扎那韦 |
P450; SARS-CoV; HIV Protease; P-gp | Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome |
Atazanavir sulfate (BMS-232632 sulfate) 是一种氮杂肽和 HIV 蛋白酶抑制剂,与其他抗 HIV 药物联合用于治疗 HIV 感染和艾滋病。它也是SARS-CoV 3CLpro 抑制剂,IC50为 3.49 μM。 | |||
T6018 |
Zosuquidar trihydrochloride
唑喹达三盐酸盐,Zosuquidar (LY335979) 3HCl,RS 33295-198 trihydrochloride,RS 33295-198 (D06387) 3HCl,Zosuquidar 3HCl,LY-335979 trihydrochloride |
P-gp | Membrane transporter/Ion channel; Neuroscience |
Zosuquidar trihydrochloride (LY-335979 trihydrochloride) 是一种P-糖蛋白抑制剂,Ki 值为 59 nM。 | |||
T74475 | m7GpppGpG | ||
m7GpppGpG 是 M7GpppNpG 三核苷酸帽类似物的一种寡核苷酸。它能够防止 5'-外切核酸酶过早的降解作用,并能够募集前 mRNA 剪接、mRNA 转运以及蛋白质生物合成启动所需的蛋白质。 | |||
T35959 |
PGPC
1-Palmitoyl-2-glutaryl phosphatidylcholine |
Others | Others |
PGPC (1-Palmitoyl-2-glutaryl phosphatidylcholine) 是一种氧化磷脂,以浓度依赖性方式激活过氧化物酶体增殖物激活受体。 | |||
T38122 |
5'-pGpG (sodium salt)
|
||
5'-pGpG is a linearized form of cyclic di-GMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3It is a metabolite of cyclic di-GMP formedviahydrolysis by various phosphodiesterases (PDEs) that binds to the cyclic di-GMP-I riboswitch with reduced affinity compared to cyclic di-GMP.4,55'-pGpG is intended for use as a negative control for cyclic di-GMP signaling. | |||
T16744 |
Rhodamine 6G
Basic Red 1,罗丹明6G,罗丹明 6G |
Others | Others |
Rhodamine 6G (Basic Red 1) 是一种罗丹明类似物,可用于表征 MRP1 介导的流出的动力学,测定 Pgp 的流出,可用作激光染料和潜在的线粒体探针。 | |||
T79261 |
P-gp inhibitor 15
|
||
P-gp inhibitor 15 (compound 7a) 是一种Pgp-非底物抑制剂,能够抑制Pgp-ATP酶的活性并干扰罗丹明123的Pgp介导外流。此外,P-gp inhibitor 15能增强紫杉醇的抗肿瘤效果,有效抑制裸鼠KBV异种移植肿瘤模型的肿瘤生长。 | |||
T12714 |
Reversan
CBLC4H10 |
Others | Others |
Reversan is a potent and nontoxic multidrug inhibitor of resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp). | |||
T33754 |
NSC-57969
NSC57969 |
||
NSC-57969 is a MDR-selective agent, exhibiting a robust Pgp-dependent toxic activity across diverse cancer cell lines. | |||
T16352 | NSC23925 | Nrf2 | Immunology/Inflammation |
NSC23925 is a selective and effective inhibitor of P-glycoprotein (Pgp). | |||
T61956 | BACE1/2-IN-1 | ||
BACE1/2-IN-1 (化合物 34) 是有效的BACE1和BACE2抑制剂,IC50分别为 0.01 和 0.0053 μM。BACE1/2-IN-1 具有较低的 Pgp 外排比和改善的被动渗透率。BACE1/2-IN-1 在肝脏微粒体中代谢稳定性降低。 | |||
T26229 |
ST7710AA1
ST-7710-AA1,ST 7710 AA1 |
||
ST7710AA1 is a PARP-1 inhibitor that acts by showing significant in vitro target inhibition and capability to substantially bypass the multidrug resistance mediated by Pgp. | |||
T68273 |
BNC105P
|
||
BNC105P is a benzofuran-based vascular disrupting agent (VDA) prodrug with potential anti-vascular and antineoplastic activities. Upon administration vascular disrupting agent BNC105P, the disodium phosphate ester of BNC105, is rapidly converted to BNC105; in activated endothelial cells, BNC105 binds to tubulin and inhibits its polymerization, which may result in a blockage of mitotic spindle formation, cell cycle arrest, and disruption of the tumor vasculature. Hypoxic conditions ensue, deprivi... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1651 |
Furanodiene
|
Apoptosis; PARP; Reactive Oxygen Species; Caspase; CDK; P-gp | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB; Proteases/Proteasome |
Furanodiene 是从姜黄中提取的一种萜类天然产物,可抑制外排转运蛋白Pgp 功能并降低 Pgp 蛋白水平。它通过抗血管生成和诱导ROS 产生,DNA 链断裂和细胞凋亡发挥抗癌作用。 | |||
T2S0223 |
Isosinensetin
异橙黄酮,6-Demethoxynobiletin |
Antioxidant; HIV Protease; Antibacterial; P-gp | Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; oxidation-reduction; Proteases/Proteasome |
Isosinensetin (6-Demethoxynobiletin) 是从青皮中提取的一种甲氧基黄酮,具有抗氧化和抑制 HIV-1 蛋白酶的活性。 | |||
T3002 |
Piperine
胡椒碱,1-Piperoylpiperidine,Bioperine |
P450; Endogenous Metabolite; P-gp; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Piperine (Bioperine) 是从胡椒中分离的一种生物碱,可以抑制P-糖蛋白和 CYP3A4 的活性,在HeLa 细胞中的IC50值为61.94±0.054 μg/mL。它已用于研究治疗多发性骨髓瘤和吞咽障碍的试验。 | |||
T3S0012 |
coniferyl ferulate
|
P-gp; GST | Membrane transporter/Ion channel; Neuroscience; oxidation-reduction |
Coniferyl ferulate 是从川芎中提取的一种天然产物,是强效的谷胱甘肽 S-转移酶抑制剂,强抑制人胎盘型谷胱甘肽 S-转移酶,IC50为 0.3 μM。它还可逆转多药耐药性并下调 P-糖蛋白。 | |||
TN4761 |
Phellamurin
|
P-gp | Membrane transporter/Ion channel; Neuroscience |
Phellamurin 是一种来自黄檗叶的黄酮糖苷,可诱导细胞凋亡,具有抗肿瘤活性。它抑制肠道 P-糖蛋白,还抑制凤蝶的产卵。 | |||
TJS1159 |
Chrysosplenetin
猫眼草黄素,Chrysosptertin B |
P450; Ferroptosis; P-gp | Apoptosis; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Chrysosplenetin 是青蒿和其他几种中草药中的一种多甲氧基化黄酮类天然产物,抑制 P-gp 活性并逆转由青蒿素诱导的上调的 P-gp 和 MDR1 水平。 | |||
T2S0271 |
Voacamine
老刺木胺,Voacanginine |
Cannabinoid Receptor; P-gp | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Voacamine (Voacanginine) 是非洲马铃果中的一种吲哚生物碱,可抑制多药耐药肿瘤细胞中的 P-糖蛋白作用,具有强效的大麻素 CB1受体拮抗活性。 | |||
T4034 |
Solamargine
Solamargin,δ-Solanigrine,澳洲茄边碱 |
Apoptosis; p38 MAPK; P-gp; STAT | Apoptosis; JAK/STAT signaling; MAPK; Membrane transporter/Ion channel; Neuroscience; Stem Cells |
Solamargine (δ-Solanigrine) 是一种来源于茄属植物的类固醇 Solasodine 的衍生物,诱导非选择性细胞毒性和 P-gp 抑制作用。它通过下调 MMP-2 和 MMP-9 的表达和活性来显著抑制 HepG2 细胞的迁移和侵袭,在多种癌症中均表现出抗癌活性。 | |||
T2S1200 |
Sinapine
|
Antioxidant; P-gp; AChE | Membrane transporter/Ion channel; Neuroscience; oxidation-reduction |
Sinapine 是萝卜中分离出来的一种生物碱,具有抗炎、抗氧化、抗肿瘤、抗血管生成和放射防护作用。它还是乙酰胆碱酯酶抑制剂,可用于研究阿尔茨海默症,共济失调,重症肌无力和帕金森氏病。 | |||
T3392 |
Sinapine thiocyanate
|
P-gp; AChE | Membrane transporter/Ion channel; Neuroscience |
Sinapine thiocyanate 是萝卜中分离出来的一种生物碱,具有抗炎、抗氧化、抗肿瘤、抗血管生成和放射防护作用。它还是乙酰胆碱酯酶抑制剂,可用于研究阿尔茨海默症,共济失调,重症肌无力和帕金森氏病。 | |||
TN1757 |
Hypophyllanthin
叶下珠次素,(7S,8S,9R)-9-(3,4-二甲氧基苯基)-6,7,8,9-四氢-4-甲氧基-7,8-双(甲氧基甲基)萘并[1,2-D]-1,3-二恶茂 |
Potassium Channel; Calcium Channel; P-gp | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Hypophyllanthin 是珠子草中的一种木脂素,能直接抑制 P-gp 的活性,具有很强的抗炎活性。 | |||
TN1525 |
Convallatoxin
K-毒毛旋花子配质-3-L-鼠李糖甙,铃兰毒苷 |
NF-κB; P-gp; PPAR | DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
Convallatoxin 是从铃兰分离得到的一种强心苷。它是 P-糖蛋白底物,并识别 Val982 是参与其转运的重要氨基酸。它是配体诱导的 MOR 胞吞作用的增强剂,通过激活PPARγ和抑制NF-κB 改善结肠炎,具有抗炎和抗增殖特性。 | |||
T2799 |
(20S)-Protopanaxadiol
20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇 |
Apoptosis; Reactive Oxygen Species; P-gp | Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) 是人参皂甙的代谢产物,是一种凋亡诱导剂,抑制Akt 活性并诱导多种肿瘤细胞凋亡。 | |||
TCS2336 |
Evodine
|
P-gp | Membrane transporter/Ion channel; Neuroscience |
Evodine 是吴茱萸中的主要柠檬苦素,是P-gp 有效抑制剂,可通过保留抗氧化剂防御系统,针对谷氨酸诱导的毒性具有保护作用。 | |||
T4085 |
Paris saponin VII
重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII |
Apoptosis; BCL; Others; PARP; p38 MAPK; Akt; Caspase; P-gp; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Membrane transporter/Ion channel; Neuroscience; Others; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Paris saponin VII (Dioscini) 是从延龄草的根和根茎中分离的一种甾体皂苷。它减弱线粒体膜电位,增加凋亡相关蛋白的表达,并降低Bcl-2、caspase-9、caspase-3、PARP-1和p-Akt 的蛋白表达水平。它在 K562/ADR 细胞中诱导强烈的自噬,可研究白血病。 | |||
TN2256 |
Taccalonolide B
根薯酮内酯B,根薯酮内酯 B |
Microtubule Associated | Cytoskeletal Signaling |
Taccalonolide B 是从广西裂果薯中分离得到的一种微管稳定剂,具有抗肿瘤活性。它抑制 SK-OV-3 细胞的生长,IC50 为 208 nM,在体外对过表达 P-糖蛋白 (Pgp) 和多药耐药蛋白 (MRP7) 的细胞系有效。 | |||
TN2254 |
Taccalonolide A
根薯酮内酯A,根薯酮内酯 A |
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Taccalonolide A 是从水田七根茎中分离得到的一种类固醇,具有细胞毒性和抗疟活性。它在体外对过表达 p 糖蛋白、多药耐药蛋白 7 细胞系有抑制作用,抑制 SK-OV-3 细胞生长的 IC50值为 622 nM。它是微管稳定剂,能引起 G2-M 期滞留、Bcl-2 磷酸化,并引发细胞凋亡。 | |||
TN4749 | Pepluanin A | P-gp | Membrane transporter/Ion channel; Neuroscience |
Pepluanin A, shows a very high activity for a jatrophane diterpene, outperforming cyclosporin A by a factor of at least 2 in the inhibition of Pgp-mediated daunomycin transport. | |||
TN4819 | (-)-Praeruptorin A | ATPase; IL Receptor; Calcium Channel; P-gp | Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
(-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings dependent on endothelium and nitric oxide synthesis;it also can significantly suppress airway inflammation and airway remodeling induced by ovalbumin challenge, and is a potential candidate for the treatment of asthma. (-)-Praeruptorin A resensitizes Pgp-mediated MDR (Pgp-MDR) cancer cells to cancer drugs. | |||
T15097 |
Deoxynivalenol
Vomitoxin,4-Deoxynivalenol |
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Deoxynivalenol (Vomitoxin) 是一种单端孢菌素家族镰刀菌属产生的霉菌毒素,常见于受到污染的食物和饲料中。Deoxynivalenol 通过紧密连接处的细胞旁路来穿过肠粘膜。Deoxynivalenol 转运不受P-糖蛋白 (PgP) 或多药耐药相关蛋白 (MRP) 抑制剂的影响。Deoxynivalenol 通常会导致人类和动物腹泻、呕吐和胃肠道炎症。 |