Membrane Transporters/Ion Channels
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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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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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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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CaCCs 抑制剂
CaCCinh-A01抑制人支气管和肠道细胞中的CaCC电流。还抑制TMEM16A通道（表达TMEM16A的FRT细胞中IC50 = 2.1 uM）。
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TMEM16A 抑制剂
T16Ainh-A01是一种选择性TMEM16A钙激活的氯离子通道抑制剂，可强烈抑制唾液腺细胞中的氯离子电流。
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Kir6.2/SUR 抑制剂
Glimepiride是一种强效Kir6.2/SUR抑制剂，SUR1、SUR2A和SURB的IC50分别为3.0 nM、5.4 nM和7.3 nM，用于治疗2型糖尿病化合物。
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Potassium Channel 抑制剂
Repaglinide是一种有效的短效胰岛素促分泌剂，可通过关闭胰岛β细胞质膜中的ATP敏感性钾（KATP）通道发挥作用。
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K+ Channel 抑制剂
K+ Channel inhibitor，Kv1.5（IKur）的二氢吡唑并嘧啶抑制剂的合成基础。
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ROMK inhibitor
MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
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hERG potassium channel inhibitor
Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
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potassium channel inhibitor
VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
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SGLT2 抑制剂
PF-04971729是钠依赖性葡萄糖共转运蛋白2的有效和选择性抑制剂。
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NMDA receptor 拮抗剂
Orphenadrine柠檬酸盐是NMDA受体拮抗剂，Ki为6.0μM，还是HERG钾离子通道阻断剂。
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PDE1 抑制剂
Vinpocetine是一种Ca2+钙调蛋白依赖性磷酸二酯酶I（PDE1）抑制剂。
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Na(+)/H(+) exchange 抑制剂
ENIPORIDE是一种有效的Na+/H+交换抑制剂。
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sodium-potassium pump 抑制剂
Digoxin是Na+/K+-ATPase 的有效抑制剂
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Sodium channel blocker/DNMT 抑制剂
Procainamide HCl是钠通道阻滞剂，又是DNA甲基转移酶抑制剂。
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sodium channel protein 抑制剂
Oxcarbazepine是一种钠通道蛋白抑制剂。
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NaV1.3 and NaV1.1 channels 抑制剂
ICA-121431是人NaV1.3和NaV1.1通道的有效和选择性抑制剂（IC50值分别为13和23 nM）。
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NBC 抑制剂
S0859是一种N-氰基磺酰胺化合物，可逆地抑制NBC介导的pH（i）恢复（K（i）= 1.7 microM，在约30 microM处完全抑制）。
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Sodium Channel 抑制剂
Sodium Channel inhibitor 1 是一种新型的选择性电压门控钠通道，用于疼痛治疗。
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late INa 抑制剂
GS967是一种新型的，有效的，选择性的心脏晚期钠电流抑制剂（INa晚期）；抑制心室肌细胞和离体心脏中ATX-II诱导的晚期I（Na），IC（50）值分别为0.13和0.21 uM。
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sodium channel 抑制剂
Levobupivacaine是属于氨基酰胺类的局部麻醉药。
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voltage-gated sodium channel 抑制剂
Procaine是具有局麻和抗心律不齐特性的苯甲酸衍生物。
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Nav1.7 抑制剂
PF-05089771是一种选择性Nav1.7抑制剂（IC50 = 11 nM），与域IV的电压传感器域（VSD）相互作用。
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Sodium Channel 抑制剂
Ambroxol HCl是神经元Na+通道的有效抑制剂，可抑制TTX耐受的Na+电流，IC50为35.2 uM，对于补品和相阻滞的IC50为22.5 μM，抑制TTX敏感的Na+电流，IC50为100 μM。第三阶段。
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- Giovanni Bocci, .et al. Virtual and In Vitro Antiviral Screening Revive Therapeutic Drugs for COVID-19, ACS Pharmacol Transl Sci, 2020, Oct 14
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voltage-gated sodium channel Nav1.7 inhibitor
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
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Sodium Channel Nav1.7 inhibitor
Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
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Nav1.7 sodium channel inhibitor
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
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Calcium Channel 抑制剂
Tetrandrine (Fanchinine)是一种钙通道阻滞剂。粉防己碱具有抗炎和抗纤维化作用，使粉防己碱及其相关化合物潜在地用于治疗肺矽肺，肝硬化和类风湿性关节炎。
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Calcium Channel 抑制剂
Nimodipine是一种L型Ca2+通道阻滞剂。
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