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Cat. No. | Product Name | Target | Signaling Pathways |
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T72521 |
Efflux inhibitor-1
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Efflux inhibitor-1为一种吡唑啉[1,5-a]嘧啶类外排抑制剂,具有对ABCG2/BCRP和ABCB1的选择性靶向性,优先靶向ABCG2,其IC50值分别为0.45 μM与2.17 μM。 | |||
T8596 |
Ceefourin 1
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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。 | |||
T1050 |
Prazosin hydrochloride
Prazosin hydrochloride,哌唑嗪盐酸盐,Prazosin HCl,cp-12299-1,Peripress,Vasoflex,盐酸哌唑嗪,Minipress |
Potassium Channel; MRP; Adrenergic Receptor; ABC; Autophagy | Autophagy; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience |
Prazosin hydrochloride (Vasoflex) 是一种选择性肾上腺素能 α-1 拮抗剂,可降低外周阻力并放松血管平滑肌。 它可用于研究高血压和酒精使用障碍。 它是一种合成哌嗪衍生物,具有降压抗肾上腺素能特性。它抑制有机阳离子转运蛋白 OCT-1 和 OCT-3,IC50分别为 1.8 和 13 μM 。 | |||
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。 | |||
T19649 |
PF-06273340
PF 6273340,PF 06273340,PF6273340,PF-6273340 |
Trk receptor | Tyrosine Kinase/Adaptors |
PF-06273340 是一种口服具有活力的、具有选择性的外周限制性Trk 泛抑制剂。 | |||
T60165 |
VB124
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Monocarboxylate transporter | Membrane transporter/Ion channel |
VB124 是一种具有口服活性的、有效且选择性的MCT4抑制剂。VB124 可特异性抑制 MDA-MB-231 细胞中乳酸的涌入和流出,IC50分别为 8.6 nM 和 19 nM。VB124 对 MCT4 的选择性高于 MCT1。VB124可用于心脏肥大、心力衰竭和代谢的研究。 | |||
T82723 |
ChTX-Lq2
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ChTX-Lq2为Ca2+激活的K+流出抑制剂,Kd值为43 nM。 | |||
T74827 |
AcrB-IN-2
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Efflux pump-IN-2 是一种 AcrB 外排泵抑制剂,能够增强抗生素的作用。Efflux pump-IN-2 抑制尼罗红 (AcrB 的一种已知底物) 外排。Efflux pump-IN-2 不破坏细菌外膜,也不会在线虫模型中显示毒性。 | |||
T14915 |
CDK12-IN-E9
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CDK | Cell Cycle/Checkpoint |
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7/CyclinH complex (IC50> 1 μM). | |||
T74828 |
AcrB-IN-3
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Efflux pump-IN-3为一种AcrB外排泵抑制剂,具有增强抗生素效力的特性。该化合物能阻断尼罗红(AcrB已知的一种底物)的外排,而不会破坏细菌的外膜,并且在线虫模型中未展现出毒性。 | |||
T81654 |
NorA-IN-1
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NorA-IN-1 (Compound 16) 为NorA抑制剂,能够抑制外翻膜囊泡中NorA外排泵的活性,适用于多药耐药性研究。 | |||
T74829 |
AcrB-IN-4
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Efflux pump-IN-4是一种针对AcrB外排泵的抑制剂,能够增强抗生素效果。该化合物通过抑制尼罗红(AcrB的已知底物)的外排来发挥作用,同时不破坏细菌外膜,且在线虫模型中未显示出毒性。 | |||
T63267 |
P-gp/BCRP-IN-1
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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。 | |||
T78200 |
BDM91270
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BDM91270(化合物 29),为大肠杆菌AcrAB-TolC外排泵抑制剂,EC90值针对野生型大肠杆菌AcrB为0.6 μM。适用于研究大肠杆菌的耐药性。 | |||
T37824 |
MCT4-IN-1
MCT4-IN-1 |
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MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research[1]. | |||
T13222 |
TTT-28
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Others | Others |
TTT-28 is a thiazole-valine peptidomimetic, and is a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocki | |||
T27211 |
DS-8587
DS 8587,DS8587,DS-8587 free |
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DS-8587 is a DNA topoisomerase inhibitor. DS-8587 exhibits potent antibacterial activity against quinolone-resistant A. baumannii isolates that harbor mutations in quinolone resistance-determining regions. DS-8587 significantly reduces the number of viabl | |||
T61956 |
BACE1/2-IN-1
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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。 | |||
T79261 |
P-gp inhibitor 15
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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。 | |||
T10453 |
BACE1-IN-5
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Beta Amyloid; BACE | Neuroscience |
BACE1-IN-5 (Compound 15) 是一种 BACE1抑制剂,IC50为 9.1 nM。BACE1-IN-5还可抑制细胞 Aβ,IC50为 0.82 nM。并且,BACE1-IN-5 具有改善 hERG 抑制和 P-gp 外排的药物化学作用。 | |||
T35568 |
BODIPY-aminoacetaldehyde diethyl acetal
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BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the effl... | |||
T72387 |
MRL-494 hydrochloride
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MRL-494 hydrochloride 是一种抗菌剂,是一种BamA 的抑制剂,具有抗外排和外膜渗透性。MRL-494 hydrochloride 可抑制革兰氏阳性细菌 (金黄色葡萄球菌 COL 的 MIC 值为 12.5 μM) 和革兰氏阴性细菌 (大肠杆菌 JCM158 的 MIC 值为 25 μM)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T80001 |
Majoranaquinone
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Antibiotic | Microbiology/Virology |
Majoranaquinone对4种Staphylococcus菌株、1种Moraxella菌株和1种Enterococcus菌株显示出良好的抑菌作用。此外,Majoranaquinone在E.coli ATCC 25922菌株中表现出显著的外排泵抑制活性,并能有效抑制E.coli ATCC 25922和E.coli K-12 AG100的生物膜形成。 |