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118

抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T21640 Talinolol

Adrenergic Receptor GPCR/G Protein; Neuroscience
Talinolol 是一种长效、心脏选择性的 β1-肾上腺素能受体阻滞剂,具有心脏保护和抗高血压作用。它也是众所周知且经常使用的 P-糖蛋白 (P-gp) 活性探针底物。
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)。
T8596 Ceefourin 1

MRP Immunology/Inflammation
Ceefourin 1 是一种具有高度选择性的多药抗性蛋白 4 (MRP4) 抑制剂。它能够抑制多种 MRP4 底物的转运,但对其他 ABC 转运蛋白无影响。它是苯并噻唑,常作为高危神经母细胞瘤的化学增敏剂。
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。
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。
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。
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。
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。
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。
TQ0311 GSK163090

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
GSK163090 是选择性和具有口服活性的5-HT1A/1B/1D 受体拮抗剂,pKi 值分别为 9.4、8.5 和 9.7。它抑制血清素再摄取转运蛋白的功能活性,pKi 值为 6.1,具有抗抑郁和抗焦虑活性。
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。
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。
T6541 Ibutilide Fumarate

Corvert Fumarate,U70226E,富马酸伊布利特

Calcium Channel; Sodium Channel Membrane transporter/Ion channel; Metabolism
Ibutilide Fumarate (U70226E) 是一种 III 类抗心律失常药物,可作用于急性心梗阻塞。
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。
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。
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。
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。
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。
T16026 MCI826

P-gp; LTR Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
MCI826 是一种具有有效性和选择性的 P-glycoprotein (P-gp)和肽白三烯 (p-LTs) 拮抗剂,在豚鼠晚期哮喘模型中显示出抗哮喘活性。
T9173 HM-30181 mesylate monohydrate

P-gp Membrane transporter/Ion channel; Neuroscience
HM-30181 mesylate monohydrate 是一种口服 P-糖蛋白 (P-gp) 抑制剂,用于提高 P-gp 底物药物的口服生物利用度。
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。
T17216 Valspodar

PSC 833

P-gp Membrane transporter/Ion channel; Neuroscience
Valspodar (PSC 833) 是一种特异性的 P-糖蛋白抑制剂和MDR调节剂,常被用作化学增敏剂,可用于研究晚期上皮卵巢癌。
T68124 Pafenolol

Adrenergic Receptor; P-gp GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
Pafenolol 是一种 P-糖蛋白调节剂,Ki 值为5.5 µM。Pafenolol 是一种可口服的且具有选择性的β肾上腺素受体拮抗剂。
T1782 Canagliflozin

卡格列净,JNJ 24831754ZAE,JNJ 28431754AAA,TA 7284,JNJ 28431754

SGLT GPCR/G Protein
Canagliflozin (JNJ 28431754AAA) 是SGLT2的选择性抑制剂,在表达 mSGLT2,rSGLT2 和 hSGLT2 的 CHO 细胞上,IC50分别为 2 nM,3.7 nM 和 4.4 nM。
T6200 Ledipasvir

GS-5885,雷迪帕韦

HCV Protease; SARS-CoV Microbiology/Virology; Proteases/Proteasome
Ledipasvir (GS-5885) 是一种丙型肝炎病毒 NS5A 抑制剂。它也是 P-糖蛋白抑制剂和乳腺癌抗性蛋白抑制剂。
T77575 P-gb-IN-1

P-gp Membrane transporter/Ion channel; Neuroscience
P-gb-IN-1 是一种有效的 P-糖蛋白 (P-gp) 抑制剂,通过抑制 P-gp 外流展现出逆转活性。P-gb-IN-1 通过与残基 Asn 721 和 Met 986 形成氢键相互作用从而显示出对 P-gp 的抑制作用。P-gb-IN-1 在 MCF-7/ADR 细胞中显示出低毒性。
T2060 ELR510444

LR-510444,LR510444,LR 510444

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
ELR510444 (LR510444) 是一种新型微管破坏剂, 抑制 MDA-MB-231 细胞增殖,IC50 为 30.9 nM。
T4595 YHO-13177

YHO 13177,YHO13177

BCRP Membrane transporter/Ion channel
YHO-13177 是高活性乳腺癌耐药蛋白多药转运通道(BCRP)抑制剂,可增强SN-38活性。
T72055 FM04

P-gp Membrane transporter/Ion channel; Neuroscience
FM04 是一种具有口服活性和高效性的 P-糖蛋白 (P-gp) 抑制剂 ,EC50 值为 83 nM。FM04 可以与人P-gp核苷酸结合域2(NBD2)中的Q1193和I1115相互作用。从而破坏 R262-Q1081-Q1118 相互作用口袋并解偶联 ICL2-NBD2 相互作用,从而抑制 P-gp。FM04 可用于癌症和肿瘤的治疗。
T64133L Laniquidar TFA

Laniquidar TFA(197509-46-9 Free base),R101933

P-gp Membrane transporter/Ion channel; Neuroscience
Laniquidar TFA (R101933) 是一种新型口服非竞争性P-糖蛋白(P-gp)抑制剂,IC50 值为 0.51 μM。Laniquidar的生物利用度有限,可用于调节多药耐药性转运体。Laniquidar可用于研究急性髓性白血病(AML)和骨髓增生异常综合征(MDS)。
T1434 Clarithromycin

A-56268,克拉霉素

P450; ribosome; MRP; Antibacterial; Antibiotic; Autophagy Autophagy; Immunology/Inflammation; Metabolism; Microbiology/Virology
Clarithromycin (A-56268) 具有广谱的抗菌活性。它抑制 CYP3A4催化的三唑仑 α-羟基化,IC50(Ki) 值为 56 (43) μM。它抑制 HERG 钾电流。它可削弱连接 hERG1 和 PI3K 的信号通路影响自噬流 。
T15713 Larotaxel

XRP9881

P-gp Membrane transporter/Ion channel; Neuroscience
Larotaxel (XRP9881) 是一种紫杉烷类似物,具有抗癌活性,通过促进微管蛋白装配和稳定微管发挥其细胞毒性作用,并通过细胞凋亡诱导细胞死亡。Larotaxel (XRP9881) 是一种可穿过血脑屏障的化合物,对 Docetaxel 的亲和力比 P-糖蛋白 1 高,可用于研究乳腺癌和膀胱癌。
T12343 Benzquinamide

BZQ,P2647,Benzoquinamide

Adrenergic Receptor GPCR/G Protein; Neuroscience
Benzquinamide (P2647) 是一种具有抗癌活性的止吐剂, 抑制p糖蛋白介导的药物外排,增强多重耐药细胞中抗癌药物的细胞毒性。Benzquinamide 对 α2A, α2B, 以及α2C 肾上腺素能受体(α2-AR)的 Ki值分别为 1,365, 691 和 545 nM。
T6075 Epothilone B

帕妥匹隆,Patupilone,EPO 906

Apoptosis; Microtubule Associated; Antibiotic; Antifungal Apoptosis; Cytoskeletal Signaling; Microbiology/Virology
Epothilone B (EPO 906) 是微管稳定剂,Ki 为0.71 μM。 它与αβ-微管蛋白异二聚体亚基结合,使αβ-微管蛋白解离减少。
T1146 Nifedipine

BAY-a-1040,Procardia XL,Procardia,硝苯地平,Adalat

CaMK; Potassium Channel; Calcium Channel; Autophagy Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience
Nifedipine (Procardia) 是一种二氢吡啶类钙通道阻滞剂,可抑制细胞外钙离子跨膜流入心肌和血管平滑肌细胞,导致主要冠状动脉和全身动脉扩张,降低心肌收缩力。它常用于心肌功能不全的相关研究。
T69515 R 101933

R 101933 is a P-glycoprotein (P-gp) inhibitor.
T14616 Biricodar

VX-710

Others Others
Biricodar is a P-glycoprotein and MRP-1 modulator.
T27985 MC-70

MC70,MC 70

MC-70 is a potent P-glycoprotein (P-gp) inhibitor (EC50 = 0.69 μM).
T12646 (R)-Verapamil hydrochloride

(R)-(+)-Verapamil hydrochloride

Others Others
(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a inhibitor of P-Glycoprotein.
T12340 P-gp modulator 1

Others Others
P-gp modulator 1 is a high affinity and orally available P-glycoprotein (Pgp) modulator
T16352 NSC23925

Nrf2 Immunology/Inflammation
NSC23925 is a selective and effective inhibitor of P-glycoprotein (Pgp).
T68737 XR9051

XR9051 is as a potent modulator of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) following a synthetic chemistry programme based on a natural product lead compound. XR9051 was shown to be a potent inhibitor of the binding of the cytotoxic to P-glycoprotein (EC50 = 1.4 +/- 0.5 nM). XR9051 reverses the MDR phenotype through direct interaction with P-glycoprotein.
T72921 Reversin 121

Reversin 121为P-糖蛋白(P-glycoprotein) 抑制剂,能增加MDR1的ATP酶活性,可逆转P-糖蛋白介导的多药耐药性,适用于癌症研究。
T29169 XR9051 Hydrochloride

XR9051 Hydrochloride, a potent modulator of P-glycoprotein-mediated multidrug resistance (MDR), inhibits the binding of cytotoxics to P-glycoprotein.
T69115 Nutlin-1

Nutlin-1 is a p53-MDM2 binding inhibitor, p-Glycoprotein (p-gp) transport substrate, and antitumor agent.

化合物

Talinolol
Cat.No: T21640
Synonym:
Target: Adrenergic Receptor
P-gp inhibitor 1
Cat.No: T12341
Synonym:
Target: Others, P-gp
Ceefourin 1
Cat.No: T8596
Synonym:
Target: MRP
Polyoxyethylene stearate
Cat.No: T16561
Synonym: POES,聚氧乙烯硬脂酸酯
Target: Antibacterial, P-gp
Dofequidar fumarate
Cat.No: T11071
Synonym: MS-209
Target: P-gp
Encequidar
Cat.No: T8426
Synonym: HM30181,HM30181A
Target: P-gp
Tariquidar
Cat.No: T6287
Synonym: XR9576,他立喹达
Target: P-gp
Selamectin
Cat.No: T4059
Synonym: UK-124114,司拉克丁,塞拉菌素
Target: Chloride channel, P-gp, Parasite
Risperidone
Cat.No: T0351
Synonym: Risperidal,R 64 766,利培酮
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, P-gp
Encequidar mesylate
Cat.No: T11578L
Synonym: HM30181 mesylate,HM30181A mesylate
Target: P-gp
Trifluoperazine
Cat.No: T8389
Synonym: 三氟拉嗪,trifluoroperazine
Target: CaMK, Dopamine Receptor, Influenza Virus, Adrenergic Receptor, P-gp, Autophagy
GSK163090
Cat.No: TQ0311
Synonym:
Target: Dopamine Receptor, 5-HT Receptor
Zamicastat
Cat.No: T13383
Synonym: BIA 5-1058
Target: BCRP, Hydroxylase, P-gp
Glibenclamide
Cat.No: T1634
Synonym: 格列本脲,Glyburide
Target: Potassium Channel, Mitochondrial Metabolism, CFTR, P-gp, Autophagy
Atazanavir
Cat.No: T0100L
Synonym: Zrivada,Reyataz,Latazanavir,阿扎那韦,BMS-232632
Target: P450, SARS-CoV, HIV Protease, P-gp
Ibutilide Fumarate
Cat.No: T6541
Synonym: Corvert Fumarate,U70226E,富马酸伊布利特
Target: Calcium Channel, Sodium Channel
Norverapamil hydrochloride
Cat.No: T16339
Synonym: (±)-Norverapamil hydrochloride,D591 hydrochloride,盐酸去甲维拉帕米
Target: Calcium Channel, P-gp, Drug Metabolite
Verapamil
Cat.No: T20656
Synonym: NSC 135784,维拉帕米,NSC-135784,CP-16533-1,(±)-Verapamil
Target: P450, Calcium Channel, P-gp
Verapamil hydrochloride
Cat.No: T1010
Synonym: Manidon,盐酸维拉帕米,(±)-Verapamil hydrochlorid,Verapamil HCl,Calcan hydrochloride
Target: P450, Calcium Channel, P-gp
Trifluoperazine dihydrochloride
Cat.No: T1222
Synonym: Trifluoperazine 2HCl,盐酸三氟拉嗪,SKF5019,Urinox
Target: CaMK, Dopamine Receptor, Influenza Virus, Adrenergic Receptor, P-gp, Autophagy
Atazanavir sulfate
Cat.No: T0100
Synonym: 阿扎那韦硫酸盐,BMS-232632,BMS-232632 sulfate,硫酸阿扎那韦
Target: P450, SARS-CoV, HIV Protease, P-gp
Elacridar
Cat.No: T2657
Synonym: GW0918,依克立达,GW120918,GF120918,GG918
Target: BCRP, P-gp
Zosuquidar trihydrochloride
Cat.No: T6018
Synonym: 唑喹达三盐酸盐,Zosuquidar (LY335979) 3HCl,RS 33295-198 trihydrochloride,RS 33295-198 (D06387) 3HCl,Zosuquidar 3HCl,LY-335979 trihydrochloride
Target: P-gp
MCI826
Cat.No: T16026
Synonym:
Target: P-gp, LTR
HM-30181 mesylate monohydrate
Cat.No: T9173
Synonym:
Target: P-gp
PGP-4008
Cat.No: T28396
Synonym: PGP 4008,PGP4008
Target: P-gp
Valspodar
Cat.No: T17216
Synonym: PSC 833
Target: P-gp
Pafenolol
Cat.No: T68124
Synonym:
Target: Adrenergic Receptor, P-gp
Canagliflozin
Cat.No: T1782
Synonym: 卡格列净,JNJ 24831754ZAE,JNJ 28431754AAA,TA 7284,JNJ 28431754
Target: SGLT
Ledipasvir
Cat.No: T6200
Synonym: GS-5885,雷迪帕韦
Target: HCV Protease, SARS-CoV
P-gb-IN-1
Cat.No: T77575
Synonym:
Target: P-gp
ELR510444
Cat.No: T2060
Synonym: LR-510444,LR510444,LR 510444
Target: Apoptosis, Microtubule Associated
YHO-13177
Cat.No: T4595
Synonym: YHO 13177,YHO13177
Target: BCRP
FM04
Cat.No: T72055
Synonym:
Target: P-gp
Laniquidar TFA
Cat.No: T64133L
Synonym: Laniquidar TFA(197509-46-9 Free base),R101933
Target: P-gp
Clarithromycin
Cat.No: T1434
Synonym: A-56268,克拉霉素
Target: P450, ribosome, MRP, Antibacterial, Antibiotic, Autophagy
Larotaxel
Cat.No: T15713
Synonym: XRP9881
Target: P-gp
Benzquinamide
Cat.No: T12343
Synonym: BZQ,P2647,Benzoquinamide
Target: Adrenergic Receptor
Epothilone B
Cat.No: T6075
Synonym: 帕妥匹隆,Patupilone,EPO 906
Target: Apoptosis, Microtubule Associated, Antibiotic, Antifungal
Nifedipine
Cat.No: T1146
Synonym: BAY-a-1040,Procardia XL,Procardia,硝苯地平,Adalat
Target: CaMK, Potassium Channel, Calcium Channel, Autophagy
R 101933
Cat.No: T69515
Synonym:
Target:
Biricodar
Cat.No: T14616
Synonym: VX-710
Target: Others
MC-70
Cat.No: T27985
Synonym: MC70,MC 70
Target:
(R)-Verapamil hydrochloride
Cat.No: T12646
Synonym: (R)-(+)-Verapamil hydrochloride
Target: Others
P-gp modulator 1
Cat.No: T12340
Synonym:
Target: Others
NSC23925
Cat.No: T16352
Synonym:
Target: Nrf2
XR9051
Cat.No: T68737
Synonym:
Target:
Reversin 121
Cat.No: T72921
Synonym:
Target:
XR9051 Hydrochloride
Cat.No: T29169
Synonym:
Target:
Nutlin-1
Cat.No: T69115
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
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。
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。
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。
T12540 Pristinamycin IA

Mikamycin IA,普利霉素IA,Mikamycin B

Others; Antibiotic; P-gp Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Others
Pristinamycin IA (Mikamycin B) 是 P-糖蛋白的底物,也是一种环肽类大环内酯抗生素。
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。
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。
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。
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。
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。
T6S1917 Schisandrol B

Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B

P450; Reactive Oxygen Species; Autophagy Autophagy; Immunology/Inflammation; Metabolism; NF-κB
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。
T3S2019 Lathyrol

Others Others
Lathyrol 是一种具有抗癌功能的天然产物。
TN5118 Taxol C

P-gp Membrane transporter/Ion channel; Neuroscience
Taxol C 可以减少与 P-糖蛋白转运蛋白的相互作用,从而增加紫杉烷类向大脑的渗透。
T6S1842 Tenacissoside G

Tenacissimoside A,通关藤苷G

Others Others
Tenacissoside G 是一种 C21 甾体,来自于Marsdenia tenacissima 茎部。它可逆转 P-糖蛋白过度表达的多药耐药癌细胞的多药耐药。
T3868 Agnuside

牡荆油,穗花牡荆苷,chasteberry oil

COX; Prostaglandin Receptor; P-gp GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
Agnuside (chasteberry oil) 是从黄荆中分离得到的一种天然产物,可下调炎性介质PGE2和LTB4,减少细胞因子的表达,具有抗关节炎活性。
TMA2270 Alisol F 24-acetate

P-gp Membrane transporter/Ion channel; Neuroscience
Alisol F 24-acetate 是一种从 Alisma plantago-aquatica Linn [1] 中分离出来的天然产物。 Alisol F 24 Acetate 通过抑制 P-糖蛋白介导的药物流出来增强 MCF-7/DOX 细胞的化学敏感性和凋亡。
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。
T6S0653 Linarin

Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷

TNF; AChE Apoptosis; Neuroscience
Linarin (Acacetin-7-O-rutinoside) 是一种选择性的乙酰胆碱酯酶 (AChE) 抑制剂,从薄荷花提取物中分离得到。
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。
T6S0119 Dauricine

蝙蝠葛碱

Apoptosis; Others; NF-κB Apoptosis; NF-κB; Others
Dauricine 是存在于北豆根粉末中的一种双苯异喹啉生物碱,具有抗炎活性。它通过抑制NF-κB 激活,剂量依赖性地抑制结肠癌细胞的增值和侵袭,并诱导凋亡。
TN5124 Taxuspine X

P-gp Membrane transporter/Ion channel; Neuroscience
Taxuspine X may have p-glycoprotein inhibitory activity.
TN5114 Taxinine

P-gp Membrane transporter/Ion channel; Neuroscience
Taxinine and Taxinine B can inhibit the drug transport by P-glycoprotein in multidrug-resistant cells.
TN1099 Dihydroevocarpine

MAO; P-gp; Antifection Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience
Dihydroevocarpine shows potent anti-Helicobacter pylori activity with the minimum inhibitory concentration (MIC) value of 10-20 microg/ml. Dihydroevocarpine is a moderate modulator of p-glycoprotein (p-gp) activity; it shows more potent inhibitory effects against MAO-B compared to MAO-A.
T72735 Coleon-U-quinone

Coleon-U-quinone 是一种有效的P-gp 抑制剂。Coleon-U-quinone 能抑制癌细胞活力,能提高多药耐药肿瘤细胞对Doxorubicin 的敏感性。
T75524 Mutabilol

Mutabilol (compound 1) 是一种有效的 p-糖蛋白 (P-gp) 调节剂。Mutabilol 是一种可以从Plectranthus mutabilis 叶中分离得到的天然产物。Mutabilol 增加 NCI-H460/R 细胞中P-gp 的表达。
TN5113 Taxinine B

Others Others
Taxinine and taxinine B can inhibit the drug transport by P-glycoprotein in multidrug-resistant cells. Taxinine B shows stronger inhibitory effects than acetylsalicylic acid (ASA) on platelet aggregation induced by arachidonic acid (AA).
T72802 Spongionellol A

Spongionellol A 是一种 MDR1(p-糖蛋白) 抑制剂。Spongionellol A 通过诱导 caspase 依赖性的凋亡 (apoptosis) 而对前列腺癌细胞具有较强的细胞毒活性和选择性。Spongionellol A 可用于癌症的研究,如前列腺癌。
T15097 Deoxynivalenol

Vomitoxin,4-Deoxynivalenol

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。
T37810 6',7'-Epoxybergamottin

6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transpo...

天然产物

Phellamurin
Cat.No: TN4761
Synonym:
Target: P-gp
Furanodiene
Cat.No: TN1651
Synonym:
Target: Apoptosis, PARP, Reactive Oxygen Species, Caspase, CDK, P-gp
coniferyl ferulate
Cat.No: T3S0012
Synonym:
Target: P-gp, GST
Isosinensetin
Cat.No: T2S0223
Synonym: 异橙黄酮,6-Demethoxynobiletin
Target: Antioxidant, HIV Protease, Antibacterial, P-gp
Piperine
Cat.No: T3002
Synonym: 胡椒碱,1-Piperoylpiperidine,Bioperine
Target: P450, Endogenous Metabolite, P-gp, Autophagy
Chrysosplenetin
Cat.No: TJS1159
Synonym: 猫眼草黄素,Chrysosptertin B
Target: P450, Ferroptosis, P-gp
Voacamine
Cat.No: T2S0271
Synonym: 老刺木胺,Voacanginine
Target: Cannabinoid Receptor, P-gp
Sinapine
Cat.No: T2S1200
Synonym:
Target: Antioxidant, P-gp, AChE
Pristinamycin IA
Cat.No: T12540
Synonym: Mikamycin IA,普利霉素IA,Mikamycin B
Target: Others, Antibiotic, P-gp
Sinapine thiocyanate
Cat.No: T3392
Synonym:
Target: P-gp, AChE
Solamargine
Cat.No: T4034
Synonym: Solamargin,δ-Solanigrine,澳洲茄边碱
Target: Apoptosis, p38 MAPK, P-gp, STAT
Hypophyllanthin
Cat.No: TN1757
Synonym: 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
Target: Potassium Channel, Calcium Channel, P-gp
Convallatoxin
Cat.No: TN1525
Synonym: K-毒毛旋花子配质-3-L-鼠李糖甙,铃兰毒苷
Target: NF-κB, P-gp, PPAR
(20S)-Protopanaxadiol
Cat.No: T2799
Synonym: 20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇
Target: Apoptosis, Reactive Oxygen Species, P-gp
Paris saponin VII
Cat.No: T4085
Synonym: 重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII
Target: Apoptosis, BCL, Others, PARP, p38 MAPK, Akt, Caspase, P-gp, Autophagy
Evodine
Cat.No: TCS2336
Synonym:
Target: P-gp
Schisandrol B
Cat.No: T6S1917
Synonym: Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B
Target: P450, Reactive Oxygen Species, Autophagy
Lathyrol
Cat.No: T3S2019
Synonym:
Target: Others
Taxol C
Cat.No: TN5118
Synonym:
Target: P-gp
Tenacissoside G
Cat.No: T6S1842
Synonym: Tenacissimoside A,通关藤苷G
Target: Others
Agnuside
Cat.No: T3868
Synonym: 牡荆油,穗花牡荆苷,chasteberry oil
Target: COX, Prostaglandin Receptor, P-gp
Alisol F 24-acetate
Cat.No: TMA2270
Synonym:
Target: P-gp
Taccalonolide B
Cat.No: TN2256
Synonym: 根薯酮内酯B,根薯酮内酯 B
Target: Microtubule Associated
Linarin
Cat.No: T6S0653
Synonym: Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷
Target: TNF, AChE
Taccalonolide A
Cat.No: TN2254
Synonym: 根薯酮内酯A,根薯酮内酯 A
Target: Apoptosis, Microtubule Associated
Dauricine
Cat.No: T6S0119
Synonym: 蝙蝠葛碱
Target: Apoptosis, Others, NF-κB
Taxuspine X
Cat.No: TN5124
Synonym:
Target: P-gp
Taxinine
Cat.No: TN5114
Synonym:
Target: P-gp
Dihydroevocarpine
Cat.No: TN1099
Synonym:
Target: MAO, P-gp, Antifection
Coleon-U-quinone
Cat.No: T72735
Synonym:
Target:
Mutabilol
Cat.No: T75524
Synonym:
Target:
Taxinine B
Cat.No: TN5113
Synonym:
Target: Others
Spongionellol A
Cat.No: T72802
Synonym:
Target:
Deoxynivalenol
Cat.No: T15097
Synonym: Vomitoxin,4-Deoxynivalenol
Target:
6',7'-Epoxybergamottin
Cat.No: T37810
Synonym:
Target:
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