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38

抑制剂 & 化合物

8

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9558 KL-11743

transporter Metabolism
KL-11743 是葡萄糖竞争性 I 类葡萄糖转运蛋白抑制剂,口服有活性,能够抑制GLUT1 (IC50:115 nM) 、GLUT2 (IC50:137 nM) 、GLUT3 (IC50:90 nM) 及GLUT4 (IC50:68 nM) 。它能够特异性阻断葡萄糖代谢,也可与电子传递抑制剂协同作用诱导细胞死亡。
T3713 BAY-876

transporter Metabolism
BAY-876 是口服有效的,选择性的葡萄糖转运蛋白 1 (GLUT1) 抑制剂(IC50= 2 nM)。BAY-876 对 GLUT1 选择性比 GLUT2,GLUT3 和 GLUT4 高(>130 倍)。BAY-876 对糖酵解代谢和卵巢癌生长也有有效的抑制作用。
T2363 STF-31

transporter; Autophagy Autophagy; Metabolism
STF31 是一种葡萄糖转运蛋白 1 的选择性抑制剂,IC50为 1 μM。
T7018 WZB117

transporter Metabolism
WZB117 是葡萄糖转运蛋白 1 抑制剂,可下调糖酵解,诱导细胞周期停滞,有抗癌细胞生长的作用。
T8616 Fasentin

N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide

transporter Metabolism
Fasentin (N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide) 是葡萄糖摄取抑制剂,可抑制GLUT-1/GLUT-4转运蛋白,优先抑制 GLUT4,IC50为 68 μM。它是死亡受体刺激敏化剂,可敏化细胞对 FAS 诱导的细胞死亡,具有抗血管生成活性。
T8732 CTPI-2

Others; Mitochondrial Metabolism Metabolism; Others
CTPI-2 是一种特异性线粒体柠檬酸盐载体SLC25A1抑制剂,KD=3.5 μM,具有抗肿瘤作用。它能够抑制糖酵解、PPARγ 及其下游靶点葡萄糖转运蛋白 GLUT4。它阻断非酒精性脂肪性肝炎逆转脂肪变性的显著改变,防止演变为脂肪性肝炎,减少肝脏和脂肪组织中炎性巨噬细胞的浸润,并显著减轻由高脂肪饮食引起的肥胖。
T4182 lavendustin B

薰草菌素B

Tyrosinase; transporter; HIV Protease Metabolism; Microbiology/Virology; Proteases/Proteasome
Lavendustin B 是一种酪氨酸激酶抑制剂,是 HIV-1 整合酶 (IN) 与其同源细胞辅助因子、晶状体上皮衍生生长因子 (LEDGF/p75) 相互作用的抑制剂。
T38843 Enavogliflozin

DWP-16001

SGLT GPCR/G Protein
Enavogliflozin (DWP-16001) 是一种口服有效的,选择性的钠-葡萄糖协同转运体 -2 抑制剂,具有抗糖尿病的功效。
T9590 T-1095

SGLT; transporter GPCR/G Protein; Metabolism
T-1095 是一种口服有活性的Na+-葡萄糖协同转运蛋白选择性抑制剂,能够抑制 SGLT1 (IC50:22.8 µm) 及 SGLT2 (IC50:2.3 µm) 。它可用于研究糖尿病。
T3547 Sotagliflozin

LX-4211,LP-802034

SGLT GPCR/G Protein
Sotagliflozin (LP-802034) 是有效的SGLT1/2抑制剂,用作抗糖尿病剂。
T22317 DRB18

transporter Metabolism
DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1/S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].
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。
T33412 MitoPQ

MitoParaquat

Glucokinase; transporter Metabolism
MitoPQ (MitoParaquat) 是一个线粒体靶向的小分子化合物。MitoPQ 选择性加强线粒体超氧化物和过氧化氢的含量,抑制胰岛素刺激的葡萄糖摄取和葡萄糖转运蛋白 4 (GLUT4) 向脂肪细胞和肌管中质膜的易位。MitoPQ 可用于研究线粒体氧化应激与调节的 GLUT4 转运。
T2389 Dapagliflozin

达格列净,BMS-512148

SGLT; HIF Angiogenesis; Chromatin/Epigenetic; GPCR/G Protein
Dapagliflozin (BMS-512148) 竞争性的葡萄糖协同转运蛋白2 (SGLT2) 抑制剂,可促进尿液中葡萄糖的排泄,在糖尿病 (DM) 研究中具有价值。Dapagliflozin 诱导 HIF1表达并减轻肾脏 IR 损伤。
T7217 Bexagliflozin

THR-1442,EGT1442,EGT0001442

SGLT GPCR/G Protein
Bexagliflozin (EGT1442) 是一种选择性的,口服有效的钠葡萄糖协同转运蛋白-2 (SGLT2) 抑制剂,对人 SGLT2 和 SGLT1 作用的 IC50值分别为 2 nM 和 5.6 μM。EGT1442在 2 型糖尿病中有研究价值。
T1782L Canagliflozin hemihydrate

JNJ28431754,TA 7284,TA7284,TA-7284,JNJ 28431754,JNJ-28431754

SGLT GPCR/G Protein
Canagliflozin hemihydrate (TA 7284) (JNJ28431754 hemihydrate) 是一种选择性的 SGLT2 抑制剂,作用于表达 mSGLT2,rSGLT2 和 hSGLT2 的 CHO 细胞,IC50 分别为 2 nM,3.7 nM 和 4.4 nM。
T16083 Mizagliflozin

GSK-1614235 free base,KGA-3235 free base,DSP-3235 free base

SGLT GPCR/G Protein
Mizagliflozin (GSK-1614235 free base) 是口服有效的、选择性的 SGLT1抑制剂,对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 对 SGLT1 的选择性是 SGLT2的303 倍。它是抗糖尿病药物,可以改善餐后血糖波动。它在改善慢性便秘方面具有潜在的作用。
T4460 Dapagliflozin ((2S)-1,2-propanediol, hydrate)

BMS-512148 (2S)-1,2-propanediol, hydrate,达格列净 (2S)-1,2-丙二醇水合物,Dapagliflozin propanediol monohydrate

SGLT GPCR/G Protein
Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) 是 Dapagliflozin 1,2-propanediol, hydrate 的 S 型异构体,是竞争性葡萄糖协同转运蛋白2 抑制剂,可促进尿液中葡萄糖的排泄,可用于糖尿病的研究。它诱导 HIF1表达并减轻肾脏 IR 损伤。
T40413 SW157765

transporter Metabolism
SW157765 是一种选择性葡萄糖转运体 GLUT8(SLC2A8)抑制剂,是很多化合物的前药,以剂量依赖性方式选择性地抑制SW157765敏感细胞中荧光 2-脱氧葡萄糖 (2DG) 的摄取 ,可用于研究肺癌。
T11420 GLUT4 activator 1

Others Others
GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).
T29188 YM-543 trimethylamine

ASP 543,ASP-543,ASP543

YM-543, a sodium-glucose transporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.
T24708 Remogliflozin

GSK189074,Remogliflozin A,GSK-189074,GSK 189074

Remogliflozin is an effective sodium-glucose transporter 2 inhibitor (Kis = 12.4 and 26 nM for human and rat SGLT2, respectively).
T12893 SGLT inhibitor-1

SGLT GPCR/G Protein
SGLT inhibitor-1 is a potentsodium glucose co-transporter proteins (SGLTs) dual inhibitor(hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively).
T10957 Dapagliflozin impurity

Others Others
Dapagliflozin impurity is the enantiomer of Dapagliflozin, Dapagliflozin is a sodium glucose transporter 2 inhibitor.
T71340 Mizagliflozin sebacate

Mizagliflozin sebacate is a sodium-glucose transporter inhibitor. It is expected to improve postprandial hyperglycemia by suppressing glucose absorption from the intestine with a novel mechanism of action different from that of conventional alpha-glucosidase inhibitors. Mizagliflozin blocks intestinal glucose absorption and reduce GIP secretion in rats and humans, suggesting SGLT1 glucose transport is critical for GIP release.
T38539 Luseogliflozin hydrate

鲁格列净水合物,TS 071 hydrate

Luseogliflozin (TS 071) hydrate, a second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor, exhibits selective potency and oral activity, with an IC50 of 2.26 nM. This compound is utilized in research for the treatment of type 2 diabetes mellitus (T2DM).
T78184 MMV009085

MMV009085是一种针对恶性疟原虫己糖转运体PfHT1的特异性抑制剂,具有潜在的抗疟效果。它同时抑制人葡萄糖转运蛋白,强效抑制葡萄糖吸收(IC50:2.6 μM)及恶性疟原虫3D7株的生长(EC50:1.23±0.04 μM)。
T36142 10-PAHSA

10-PAHSA is a newly identified endogenous lipid that belongs to a collection of branched fatty acid esters of hydroxy fatty acids (FAHFAs). It is a FAHFA in which palmitic acid is esterified to 10-hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. As other FAHFAs improve glucose tolerance, stimulate insulin secretion, and have anti-...
T82294 GLUT1-IN-3

GLUT1-IN-3 (Compd 4b) 是针对1型葡萄糖转运蛋白缺乏综合症相关疾病研究的化合物,具有有效抑制癫痫发作的作用。
T79263 Antitumor agent-102

Topoisomerase DNA Damage/DNA Repair
Antitumor agent-102(compound 10)是拓扑异构酶 I(topoisomerase I)抑制剂SN38与葡萄糖转运蛋白(glucose transporter)抑制剂缀合物,专门针对结直肠癌。相较于伊立替康,该化合物在肿瘤组织中可诱导游离SN38的更高浓度。
T37118 ADP-Glucose (sodium salt)

ADPG,Adenosine-5'-diphosphoglucose,ADP-Glucose (sodium salt)

ADP-Glucose (ADPG) is an immediate precursor used in the biosynthesis, by glucose addition, of storage polysaccharides in plants, green algae, and cyanobacteria, as well as structural polysaccharides in certain bacteria.[1],[2] It is used by amylose synthases or starch synthases in plastids in the production of amylose, amylopectins, starch, and other polysaccharides. ADPG is normally generated within plastids, although it can be biosynthesized in the cytoplasm of certain grasses and imported in...
T70390 YM-543 choline

YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose level...
T69622 Ritivixibat

Ritivixibat为回肠胆汁酸转运蛋白(IBAT)抑制剂,同时也是胆汁酸调节剂,主要适用于心血管疾病、脂肪酸代谢及葡萄糖利用障碍、胃肠道和肝脏疾病的研究。
T60629 PF-06649298

PF-06649298 是一种钠偶联柠檬酸盐转运蛋白抑制剂,可用于调节糖代谢以及脂代谢的研究。PF-06649298 在人类肝细胞中与 NaCT 特异性结合从而抑制柠檬酸盐的转运,IC50值为 16.2 μM。
T71981 Gliclazide-d4

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin...
T73734 Acetoacetic acid

Acetoacetic acid是一种存在于脑脊液中的内源代谢物,主要应用于脑膜炎、妊娠、3-羟基-3-甲基戊二酰辅酶A裂解酶缺乏症、子痫前期/子痫、2型糖尿病、1型葡萄糖转运蛋白缺乏综合征及琥珀酰辅酶A:3-氧酸辅酶A转移酶缺乏症的研究中。
T36586 12-PAHSA

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to either a C-16 or C-18 hydroxy substituent. 12-PAHSA is a FAHFA in which palmitic acid is esterified at the 12th carbon of hydroxy stearic acid. Among the FAHFA family members, PAHSAs ar...
T74962 GLUT1-IN-1

GLUT1-IN-1 是一种GLUT1 (葡萄糖转运蛋白 1) 抑制剂,显著特异性地失活GLUT1。该化合物对HeLa、A549 及HepG2 细胞线呈现浓度依赖性的细胞毒性,其IC50 值分别为5.49 μM、11.14 μM 与8.73 μM。GLUT1-IN-1 主要应用于光动力疗法(PDT)与癌症研究领域。

化合物

KL-11743
Cat.No: T9558
Synonym:
Target: transporter
BAY-876
Cat.No: T3713
Synonym:
Target: transporter
STF-31
Cat.No: T2363
Synonym:
Target: transporter, Autophagy
WZB117
Cat.No: T7018
Synonym:
Target: transporter
Fasentin
Cat.No: T8616
Synonym: N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
Target: transporter
CTPI-2
Cat.No: T8732
Synonym:
Target: Others, Mitochondrial Metabolism
lavendustin B
Cat.No: T4182
Synonym: 薰草菌素B
Target: Tyrosinase, transporter, HIV Protease
Enavogliflozin
Cat.No: T38843
Synonym: DWP-16001
Target: SGLT
T-1095
Cat.No: T9590
Synonym:
Target: SGLT, transporter
Sotagliflozin
Cat.No: T3547
Synonym: LX-4211,LP-802034
Target: SGLT
DRB18
Cat.No: T22317
Synonym:
Target: transporter
Canagliflozin
Cat.No: T1782
Synonym: 卡格列净,JNJ 24831754ZAE,JNJ 28431754AAA,TA 7284,JNJ 28431754
Target: SGLT
MitoPQ
Cat.No: T33412
Synonym: MitoParaquat
Target: Glucokinase, transporter
Dapagliflozin
Cat.No: T2389
Synonym: 达格列净,BMS-512148
Target: SGLT, HIF
Bexagliflozin
Cat.No: T7217
Synonym: THR-1442,EGT1442,EGT0001442
Target: SGLT
Canagliflozin hemihydrate
Cat.No: T1782L
Synonym: JNJ28431754,TA 7284,TA7284,TA-7284,JNJ 28431754,JNJ-28431754
Target: SGLT
Mizagliflozin
Cat.No: T16083
Synonym: GSK-1614235 free base,KGA-3235 free base,DSP-3235 free base
Target: SGLT
Dapagliflozin ((2S)-1,2-propanediol, hydrate)
Cat.No: T4460
Synonym: BMS-512148 (2S)-1,2-propanediol, hydrate,达格列净 (2S)-1,2-丙二醇水合物,Dapagliflozin propanediol monohydrate
Target: SGLT
SW157765
Cat.No: T40413
Synonym:
Target: transporter
GLUT4 activator 1
Cat.No: T11420
Synonym:
Target: Others
YM-543 trimethylamine
Cat.No: T29188
Synonym: ASP 543,ASP-543,ASP543
Target:
Remogliflozin
Cat.No: T24708
Synonym: GSK189074,Remogliflozin A,GSK-189074,GSK 189074
Target:
SGLT inhibitor-1
Cat.No: T12893
Synonym:
Target: SGLT
Dapagliflozin impurity
Cat.No: T10957
Synonym:
Target: Others
Mizagliflozin sebacate
Cat.No: T71340
Synonym:
Target:
Luseogliflozin hydrate
Cat.No: T38539
Synonym: 鲁格列净水合物,TS 071 hydrate
Target:
MMV009085
Cat.No: T78184
Synonym:
Target:
10-PAHSA
Cat.No: T36142
Synonym:
Target:
GLUT1-IN-3
Cat.No: T82294
Synonym:
Target:
Antitumor agent-102
Cat.No: T79263
Synonym:
Target: Topoisomerase
ADP-Glucose (sodium salt)
Cat.No: T37118
Synonym: ADPG,Adenosine-5'-diphosphoglucose,ADP-Glucose (sodium salt)
Target:
YM-543 choline
Cat.No: T70390
Synonym:
Target:
Ritivixibat
Cat.No: T69622
Synonym:
Target:
PF-06649298
Cat.No: T60629
Synonym:
Target:
Gliclazide-d4
Cat.No: T71981
Synonym:
Target:
Acetoacetic acid
Cat.No: T73734
Synonym:
Target:
12-PAHSA
Cat.No: T36586
Synonym:
Target:
GLUT1-IN-1
Cat.No: T74962
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1118 Tormentic acid

2Α,19Α-二羟基熊果酸,委陵菜酸

Immunology/Inflammation related Immunology/Inflammation
Tormentic acid 是一种分离自 Rosa rugosa 中的三萜,具有抗炎、降血脂和抗动脉粥样硬化活性。
T4S1545 Licarin B

(-)-Licarin B,Licarine B,(-)-利卡灵B

transporter; Antibacterial; PPAR DNA Damage/DNA Repair; Metabolism; Microbiology/Virology
Licarin B (Licarine B) 是来源于肉豆蔻种子的一种天然产物,是 NO 生成抑制剂,可通过激活 IRS-1/PI3K/AKT 通路中的PPARγ和GLUT4 改善胰岛素敏感性。
T2924 Phloretin

根皮素,Dihydronaringenin,NSC 407292,RJC 02792

SGLT; transporter; Endogenous Metabolite GPCR/G Protein; Metabolism
Phloretin (NSC-407292) 是从苹果树叶中提取的一种查耳酮,具有抗炎、抗氧化和抗癌活性。它是真核尿素转运蛋白抑制剂,可阻断 VacA 介导的尿素和离子转运,有潜力用于类风湿性关节炎和过敏性气道炎症的相关研究。
T6S0117 Avicularin

Fenicularin,扁蓄苷

ERK MAPK
Avicularin (Fenicularin) 具有抗过敏、抗炎、保肝、抗氧化、抗肿瘤等活性。它能通过调节 NF-κB(p65)、COX-2 和 PPAR-γ 的活性来改善人类肝细胞癌。在 LPS 刺激的 RAW 264.7 巨噬细胞中,它通过抑制 ERK 信号通路产生抗炎活性。
TN1034 Sennidin B

HCV Protease; transporter; Akt; PI3K Cytoskeletal Signaling; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
Sennidin B 是从Cassia angustifolia 分离得到的Sennidin A 异构体,它刺激葡萄糖掺入,诱导Akt 和葡萄糖转运蛋白4 的磷酸化。
TN1033 Sennidin A

HCV Protease; transporter; Akt; PI3K Cytoskeletal Signaling; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
Sennidin A 是从狭叶番泻分离得到的一种天然产物,能够抑制 HCV NS3 解旋酶,其 IC50值为0.8 μM。它诱导 Akt 和葡萄糖转运蛋白4的磷酸化,刺激葡萄糖掺入。
T2755 Rhoifolin

野漆树苷,Apigenin-7-O-rhamnoglucoside,Apigenin 7-O-neohesperidoside,Rhoifoloside

Others; p38 MAPK; NF-κB; transporter; IGF-1R; Autophagy Autophagy; MAPK; Metabolism; NF-κB; Others; Tyrosine Kinase/Adaptors
Rhoifolin (Apigenin 7-O-neohesperidoside) 是从琯溪蜜柚叶子分离的一种黄酮糖苷。它通过 RANKL 诱导的NF-κB 和MAPK 途径改善钛颗粒刺激的骨溶解并减少破骨细胞生成。它通过增强脂联素分泌,胰岛素受体-β的酪氨酸磷酸化和GLUT4易位有助于治疗糖尿病并发症。
T72172 4,6-O-Ethylidene-α-D-glucose

Ethylidene-glucose

4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose) 是一种葡萄糖衍生物,是竞争性的葡萄糖转运蛋白 1 (GLUT1) 面部结合部位抑制剂,对野生型 2-脱氧-D-葡萄糖转运的 Ki 值为 12 mM。

天然产物

Tormentic acid
Cat.No: TN1118
Synonym: 2Α,19Α-二羟基熊果酸,委陵菜酸
Target: Immunology/Inflammation related
Licarin B
Cat.No: T4S1545
Synonym: (-)-Licarin B,Licarine B,(-)-利卡灵B
Target: transporter, Antibacterial, PPAR
Phloretin
Cat.No: T2924
Synonym: 根皮素,Dihydronaringenin,NSC 407292,RJC 02792
Target: SGLT, transporter, Endogenous Metabolite
Avicularin
Cat.No: T6S0117
Synonym: Fenicularin,扁蓄苷
Target: ERK
Sennidin B
Cat.No: TN1034
Synonym:
Target: HCV Protease, transporter, Akt, PI3K
Sennidin A
Cat.No: TN1033
Synonym:
Target: HCV Protease, transporter, Akt, PI3K
Rhoifolin
Cat.No: T2755
Synonym: 野漆树苷,Apigenin-7-O-rhamnoglucoside,Apigenin 7-O-neohesperidoside,Rhoifoloside
Target: Others, p38 MAPK, NF-κB, transporter, IGF-1R, Autophagy
4,6-O-Ethylidene-α-D-glucose
Cat.No: T72172
Synonym: Ethylidene-glucose
Target:
TargetMol Loading
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