Membrane Transporters/Ion Channels
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VMAT2 抑制剂
GZ-793A是囊泡单胺转运蛋白2 (VMAT2)的选择性抑制剂，它将单胺神经递质从细胞胞质溶胶转运到突触小泡中。
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VMAT2 抑制剂
Valbenazine是一种有效的选择性VMAT2抑制剂。
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NHE3 抑制剂
Tenapanor充当钠-质子交换器NHE3的抑制剂。这种抗转运蛋白在肾脏和肠道中发现，通常起到调节机体吸收和分泌的钠水平的作用。
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- Xingjie Tan, .et al. The Na+/H+ exchanger NHE3 inhibitor tenapanor prevents intestinal obstructions in CFTR-deleted mice, Authorea, 2022, May 25
- Kunyan Zhou, .et al. Functional characterization of the sodium/hydrogen exchanger 8 and its role in proliferation of colonic epithelial cells, Am J Physiol Cell Physiol, 2021, Sep 1;321(3):C471-C488 PMID: 34288721
- Qinghai Tan, .et al. Inhibition of Na + /H + exchanger isoform 3 improves gut fluidity and alkalinity in cystic fibrosis transmembrane conductance regulator-deficient and F508del mutant mice, Br J Pharmacol, 2021, Mar;178(5):1018-1036 PMID: 33179259
- Y Liu, .et al. Deciphering Ion Transporters, Kinases and PDZ-adaptor Molecules That Mediate Guanylate Cyclase C Agonist-Dependent Intestinal Fluid Loss in Vivo, Biochem Pharmacol, 2020, May 16;178:114040 PMID: 32422138
- Yu Y, .et al. Expression, Localization and Functional Activity of the Major Na+/H+ Exchange Isoforms Expressed in the Intestinal Cell Line Caco-2BBe, Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thammayon N, .et al. Na+/H+ exchanger 3 inhibitor diminishes the amino-acid-enhanced transepithelial calcium transport across the rat duodenum, Amino Acids, 2017, Apr;49(4):725-734 PMID: 27981415
- Charoenphandhu N, .et al. Na+/H+ exchanger 3 inhibitor diminishes hepcidin-enhanced duodenal calcium transport in hemizygous β-globin knockout thalassemic mice, Mol Cell Biochem, 2017, Mar;427(1-2):201-208 PMID: 27995414
- Jantarajit W, .et al. CFTR-mediated anion secretion across intestinal epithelium-like Caco-2 monolayer under PTH stimulation is dependent on intermediate conductance K+ channels, Am J Physiol Cell Physiol, 2017, Jul 1;313(1):C118-C129 PMID: 28490422
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NHE-1 inhibitor
Rimeporide(EMD-87580)是Na+/H+交换剂（NHE-1）的有效和选择性抑制剂。
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NHE3 抑制剂
NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
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BCRP 抑制剂
ko 143是有效的选择性乳腺癌耐药蛋白多药转运蛋白(BCRP)抑制剂，EC90值为26 nM。
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BCRP/ABCG2 抑制剂
YHO-13177是一种有效且特异性的乳腺癌抗性蛋白（BCRP/ABCG2）抑制剂。
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BCRP inhibitor
YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
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Na+/Ca2+ Exchanger 抑制剂
KB-R7943 mesylate是一种在表达NCX1的细胞中具有Na+/Ca2+交换反向模式的细胞渗透性强效选择性NCKX抑制剂。
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NCX 抑制剂
SEA0400是Na+-Ca2+交换剂的新型选择性抑制剂，IC50为5-33 nM（抑制培养的神经元，星形胶质细胞和小胶质细胞中Na+依赖的Ca2+吸收。
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- Wakana Shoda, .et al. Sodium-calcium exchanger 1 is the key molecule for urinary potassium excretion against acute hyperkalemia, PLoS One, 2020, 15(6): e0235360 PMID: 32603346
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Na+/Ca2+ exchange 抑制剂
CGP 37157是苯并硫氮平，可作为线粒体钠钙交换剂的选择性抑制剂（在分离的线粒体中IC50 = 0.36 μM）。
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Na+/Ca2+ exchanger (NCX) 抑制剂
ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC50s of 55 and 67 nM at -80 and at 20 mV, respectively.
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NCX inhibitor
ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively.
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proton pump 抑制剂
Tenatoprazole是质子泵抑制剂（PPI）类的前药，可抑制质子转运，IC50为3.2 uM。
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Proton pump 抑制剂
Esomeprazole Magnesium trihydrate 是质子泵抑制剂，可通过抑制胃壁细胞中的H+/K+ ATPase来减少酸的分泌。
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Proton pump 抑制剂
Esomeprazole sodium是一种质子泵抑制剂，可通过抑制胃壁细胞中的H+/K+ ATPase来减少酸的分泌。
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proton pump 抑制剂
Rebeprazole sodium是质子泵抑制剂中的一种抗溃疡药。
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Proton pump 抑制剂
Lauric acid是质子泵抑制剂，可能用于治疗幽门螺杆菌感染。
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SNR 抑制剂
Sibutramine hydrochloride是5-HT和去甲肾上腺素再摄取抑制剂（SNRI）。
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Serotonin transporter 抑制剂
Imipramine Hydrochloride是一种三环抗抑郁药。抑制血清素和去甲肾上腺素转运蛋白，但对多巴胺转运蛋白几乎没有影响。
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serotonin reuptake 抑制剂
Azaphen dihydrochloride monohydrate是5-羟色胺再摄取的有效抑制剂。
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EAAT1 抑制剂
UCPH 101是EAAT1的选择性非底物抑制剂（EAAT1，EAAT2和EAAT3的IC50分别为660，> 300000和> 300000 nM）。
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TRPA1 抑制剂
HC-030031是选择性TRPA1阻滞剂，可拮抗AITC和福尔马林诱导的TRPA1介导的钙内流（IC50分别为6.2和5.3 uM）。
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TRPC4/C5 抑制剂
ML204是一种新型强效拮抗剂，可选择性调节天然TRPC4/C5离子通道。
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TRPC6 inhibitor
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
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TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
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TRPC1/4/5 channels inhibitor
Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
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TRPC6 inhibitor
SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
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TRPC3 inhibitor
Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
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CRM1 抑制剂
KPT185是选择性CRM1抑制剂。KPT-185以100 nM至500 nM的IC50显着抑制白血病细胞增殖，并诱导AML细胞系和原发性AML原始细胞的细胞周期停滞和凋亡。
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CRM1 抑制剂
CRM1（XPO1）介导的核输出的KPT-330抑制剂在T细胞急性淋巴细胞白血病和急性骨髓性白血病的临床前模型中具有选择性的抗白血病活性。
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- Chie Ishikawa, .et al. Exportin-1 is critical for cell proliferation and survival in adult T cell leukemia, Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
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SINE/CRM1 抑制剂
KPT276是KPT-185的类似物，是核出口（SINE）和CRM1的选择性抑制剂。
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CRM1 inhibitor
Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.
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nuclear export receptor CRM1 inhibitor
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
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MDR1/P-gp 抑制剂
PSC-833 (Valspodar)是一种P-糖蛋白（P-gp）调节剂，可抑制P-gp介导的多药耐药性（MDR）。
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- Somin Lee, .et al. BBB-on-a-Chip: Modeling Functional Human Blood-Brain Barrier by Mimicking 3D Brain Angiogenesis Using Microfluidic Chip, Methods Mol Biol, 2022, 2492:251-263 PMID: 35733049
- Somin Lee, .et al. 3D brain angiogenesis model to reconstitute functional human blood?Cbrain barrier in vitro, ?Biotechnol Bioeng, 2019, 10 November
- Somin Lee, .et al. 3D brain angiogenesis model to reconstitute maturation of functional human blood-brain barrier in vitro, bioRxiv, 2018, Nov. 18
- Watanabe N, .et al. The possible clinical impact of risperidone on P-glycoprotein-mediated transport of tacrolimus: A case report and in vitro study, Biopharm Drug Dispos, 2018, Jan;39(1):30-37 PMID: 29055041
- Higashi H, .et al. In Vitro P-Glycoprotein-Mediated Transport of Tadalafil: A Comparison with Sildenafil, Biol Pharm Bull, 2017, 40(8):1314-1319 PMID: 28769012
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P-gp & BCRP 抑制剂
Elacridar (GF120918)是一种原型BCRP抑制剂，可抑制Bcrp1介导的转运。
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- Leo Shen, .et al. A forward genetic screen identifies modifiers of rocaglate responsiveness, Sci Rep, 2021, Sep 16;11(1):18516 PMID: 34531456
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P-gp 抑制剂
Tariquidar (XR9576)是一种P-糖蛋白药物外排泵抑制剂。
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- Yuko Sasaki, .et al. Intestinal Permeability of Drugs in Caco-2 Cells Cultured in Microfluidic Devices, Biol Pharm Bull, 2022, 45(9):1246-1253 PMID: 36047192
- Sugisawa N, .et al. Novel Potent ABCB1 Modulator, Phenethylisoquinoline Alkaloid, Reverses Multidrug Resistance in Cancer Cell, Mol Pharm, 2018, Sep 4;15(9):4021-4030 PMID: 30052463
- Samy A. F. Morad, .et al. Role of P-glycoprotein inhibitors in ceramide-based therapeutics for treatment of cancer, Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Debora Petroni, .et al. Synthesis and In Vivo Imaging of N-(3-[11C]Methoxybenzyl)-2-(3-Methoxyphenyl)ethylaniline as a Potential Targeting Agent for P-glycoprotein, Mol Imaging Biol, 2016, Dec;18(6):916-923 PMID: 27234445
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P-glycoprotein 抑制剂
XR9576是一种 P-glycoprotein (P-gp) 抑制剂，Kd值为5.1 nM。正在研究中作为抗癌多药耐药性的佐剂。
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P-gp 抑制剂
ONT-093是口服可生物利用的P-糖蛋白泵抑制剂，可潜在逆转接受癌症化学疗法的患者的多药耐药性。
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P-gp 抑制剂
Laniquidar是第三代P-gp抑制剂，已在临床试验中用于调节多药耐药转运蛋白。
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P-gp 抑制剂
MC 70 HCl是有效的P-gp抑制剂（EC50 = 0.69 uM）。
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BCRP 抑制剂
KS-176是乳腺癌抗性蛋白（BCRP）多药转运蛋白的有效和选择性抑制剂（在Pheo A和Hoechst 33342分析中，IC50值分别为0.59和1.39 uM）。
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P-gp/BCRP dual 抑制剂
FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
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P-gp 抑制剂
Elacridar hydrochloride是一种P-糖蛋白抑制剂，已在体内和体外用作P-糖蛋白（Pgp）的工具抑制剂，以研究转运蛋白在处理各种测试分子中的作用。
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P-gp 抑制剂
Zosuquidar是P-糖蛋白介导的多药耐药性的有效调节剂，Ki为60 nM。
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ABCB1 (P-gp/MDR1) inhibitor
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity.
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P-gp inhibitor
Norverapamil hydrochloride ((??)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
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P-gp inhibitor
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
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AMPA Receptor 抑制剂
Aniracetam是一种安非他命，属于消旋体化学类别的促智药，据称比吡乙酰胺更有效。
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AMPA desensitization 抑制剂
Cyclothiazide是苯并噻二叠氮，可作为AMPA受体的增效剂，正向调节其对谷氨酸的响应（EC50 = 3.8 M）。
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