Membrane Transporters/Ion Channels
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SGLT2 抑制剂
Dapagliflozin (BMS512148)抑制钠-葡萄糖转运蛋白（SGLT2）的亚型2，后者负责肾脏中至少90％的葡萄糖重吸收。
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- David Papadopoli, .et al. Perturbations of cancer cell metabolism by the antidiabetic drug canagliflozin, Neoplasia, 2021, Apr;23(4):391-399 PMID: 33784591
- Neil Tanday, .et al. Dapagliflozin exerts positive effects on beta cells, decreases glucagon and does not alter beta- to alpha-cell transdifferentiation in mouse models of diabetes and insulin resistance, Biochem Pharmacol, 2020, Jul;177:114009 PMID: 32360307
- Subramaniam M, .et al. Comparison of Intestinal Glucose Flux and Electrogenic Current Demonstrates Two Absorptive Pathways in Pig and One in Nile Tilapia and Rainbow Trout, Am J Physiol Regul Integr Comp Physiol, 2019, Nov 20 PMID: 31746628
- Marina Subramaniam, .et al. Sigmoidal kinetics define porcine intestinal segregation of electrogenic monosaccharide transport systems as having multiple transporter population involvement, Physiol Rep, 2019, May; 7(9): e14090 PMID: 31062524
- Angelopoulou A, .et al. Magnetic Nanoparticles for the Delivery of Dapagliflozin to Hypoxic Tumors: Physicochemical Characterization and Cell Studies, AAPS PharmSciTech, 2018, Feb;19(2):621-633 PMID: 8924948
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SGLT2 抑制剂
canagliflozin是2型亚钠葡萄糖转运蛋白（SGLT2）的抑制剂,作用于hSGLT2，无细胞试验中IC50为2.2 nM，比作用于hSGLT1选择性高413倍。
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- David Papadopoli, .et al. Perturbations of cancer cell metabolism by the antidiabetic drug canagliflozin, Neoplasia, 2021, Apr;23(4):391-399 PMID: 33784591
- Angelopoulou A, .et al. Canagliflozin-loaded magnetic nanoparticles as potential treatment of hypoxic tumors in combination with radiotherapy, Nanomedicine, 2018, Oct;13(19):2435-2454 PMID: 30311542
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SGLT2 抑制剂
EGT1442是有效的选择性SGLT2抑制剂。
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SGLT 抑制剂?
LX4211是双重SGLT1/SGLT2抑制剂。
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SGLT2 抑制剂
Tofogliflozin是亚型2钠葡萄糖转运蛋白（SGLT2）的抑制剂，可引起肾脏中至少90％的葡萄糖重吸收。
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SGLT2 抑制剂
Remogliflozin抑制钠葡萄糖转运蛋白（SGLT2），后者负责肾脏中的葡萄糖重吸收。
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SGLT2 抑制剂
Ipragliflozin是一种高效的选择性SGLT2抑制剂，IC50为2.8 nM。SGLT1/3/4/5/6的效力很小且没有效力。
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SGLT2 抑制剂
Luseogliflozin是由Taisho Pharmaceutical开发的一种口服活性第二代钠葡萄糖共转运蛋白2（SGLT2）抑制剂，用于治疗2型糖尿病（T2DM）患者。
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Na+-glucose transporter 抑制剂
T-1095是Na+-葡萄糖共转运蛋白（SGLTs）的有效和选择性抑制剂。
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SGLT2 抑制剂
Canagliflozin hemihydrate是半水形式的卡格列嗪，是一种SGLT2抑制剂，在无细胞检测中hSGLT2的IC50为2.2 nM，其选择性比hSGLT1高413倍。
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SGLT inhibitor
Ertugliflozin pidolate belongs to the class of potent and selective inhibitors of the sodium-dependent glucose cotransporters (SGLT), more specifically the type 2 which is responsible for about 90% of the glucose reabsorption from glomerulus.
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SGLT1 抑制剂
SGL5213 is a potent, oral active and low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor, with IC50 values of 29 nM and 20 nM for hSGLT1 and hSGLT2, respectively.
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SGLT2 抑制剂
Dapagliflozin impurity is an enantiomer of Dapagliflozin which is a sodium-glucose transporter 2 inhibitor.
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SGLT1/SGLT2 抑制剂
Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
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MCT1 inhibitor
BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
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MCT1 and MCT2 抑制剂
AR-C155858是单羧酸转运蛋白mct1和mct2的有效抑制剂，它们与涉及跨膜螺旋7-10的细胞内位点结合。
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- Charlotte Petersen, .et al. MCT1 and MCT4 Expression and Lactate Flux Activity Increase During White and Brown Adipogenesis and Impact Adipocyte Metabolism, Sci Rep, 2017, 7: 13101 PMID: 29026134
- Kong SC, .et al. Monocarboxylate Transporters MCT1 and MCT4 Regulate Migration and Invasion of Pancreatic Ductal Adenocarcinoma Cells, Pancreas, 2016, Aug;45(7):1036-47 PMID: 26765963
- Anne Poder, .et al. Roles of acid-extruding ion transporters in regulation of breast cancer cell growth in a 3-dimensional microenvironment, Mol Cancer, 2016, 15: 45 PMID: 27266704
- Eumorphia G. Konstantakou, .et al. 3-BrPA eliminates human bladder cancer cells with highly oncogenic signatures via engagement of specific death programs and perturbation of multiple signaling and metabolic determinants, Mol Cancer, 2015, 14: 135 PMID: 26198749
- Álvarez Z, .et al. Neurogenesis and vascularization of the damaged brain using a lactate-releasing biomimetic scaffold., Biomaterials., 2014, 35(17):4769-81 PMID: 24636215
- Álvarez Z, .et al. Neuronal Progenitor Maintenance Requires Lactate Metabolism and PEPCK-M-Directed Cataplerosis., Cereb Cortex., 2014, 26(3):1046-58 PMID: 25452568
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MCT 抑制剂
CHC是单羧酸转运（MCT）抑制剂。在神经胶质瘤中具有抗肿瘤和抗血管生成活性；降低U251细胞的糖酵解代谢，迁移和侵袭。
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MCT1 抑制剂
AZD-3965（AZD3965）是具有1.6 nM结合亲和力的单羧酸盐转运蛋白1（MCT1）的选择性抑制剂，是MCT2的6倍选择性，在10μM时不抑制MCT4。
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- Lu Gao, .et al. Trophoblast-derived Lactic Acid Orchestrates Decidual Macrophage Differentiation via SRC/LDHA Signaling in Early Pregnancy, Int J Biol Sci, 2022, Jan 1;18(2):599-616 PMID: 35002512
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MCT1 抑制剂
AR-C117977是一种有效的MCT1抑制剂，可以降低体内和体外的免疫应答，维持长期移植物存活，并诱导操作耐受性。
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MCT 抑制剂
7ACC2是一种新型有效的MCT抑制剂，IC50为11 nM，可抑制[14C]-乳酸盐涌入。针对癌细胞中乳酸转运的新型抗肿瘤治疗。
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MCT 抑制剂?
7ACC1在富含乳酸的肿瘤微环境中选择性干扰乳酸通量；在表达MCT1和MCT4转运蛋白的肿瘤细胞中，乳酸抑制乳酸盐流入，但不流出。
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- Daniel Gundel, .et al. Preclinical Evaluation of [18F]FACH in Healthy Mice and Piglets: An 18F-Labeled Ligand for Imaging of Monocarboxylate Transporters with PET, Int J Mol Sci, 2021, Feb; 22(4): 1645 PMID: 33562048
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MCT 抑制剂
UK 5099是质膜单羧酸盐转运蛋白（MCT）和线粒体丙酮酸载体（MPC）的有效抑制剂。抑制丙酮酸依赖性的氧气消耗，IC50为50 nM。
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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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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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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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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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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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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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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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