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39

抑制剂 & 化合物

5

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Cat. No. Product Name Target Signaling Pathways
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。
T2385 Ipragliflozin

伊格列净,ASP1941

SGLT GPCR/G Protein
Ipragliflozin (ASP1941) 是一种口服有效的,选择性的 SGLT2抑制剂,对人 SGLT2SGLT1,大鼠 SGLT2SGLT1,小鼠 SGLT2SGLT1 的 IC50分别为 7.38 和 1876 nM,6.73 和 1166 nM,5.64 和 1380 nM。Ipragliflozin 具有抗糖尿病活性。
T4999 Ertugliflozin

埃格列净,MK-8835,PF-04971729

SGLT GPCR/G Protein
Ertugliflozin (PF-04971729) 是选择性的、口服有效的钠离子依赖的葡萄糖协同转运蛋白2 (SGLT2) 抑制剂,对h-SGLT2 的IC50值为 0.877 nM。Ertugliflozin 在2型糖尿病中有研究价值。
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。
T34286 Remogliflozin etabonate

GSK189075,GSK 189075,GSK-189075A,GSK189075A,GSK-189075,GSK 189075A

SGLT GPCR/G Protein
Remogliflozin etabonate (GSK189075A) 是 regaliflozin 的前药和 SGLT2 抑制剂,对 hSGLT2、rSGLT2、rSGLT1 和 hSGLT1 的 Ki 值分别为 1.95、2.14、8.57 和 43.1μM。
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。
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。
T67849 O-Desethyl Dapagliflozin

Empagliflozin-4

SGLT GPCR/G Protein
O-Desethyl Dapagliflozin (Empagliflozin-4) 是一种 SGLT2 抑制剂, IC50=33nM.
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 SGLT2SGLT1 作用的 IC50值分别为 2 nM 和 5.6 μM。EGT14422 型糖尿病中有研究价值。
T5016 Tofogliflozin (hydrate)

托格列净,Tofogliflozin hydrate,CSG-452 hydrate

SGLT; Reactive Oxygen Species; ROS GPCR/G Protein; Immunology/Inflammation; Metabolism; NF-κB
Tofogliflozin hydrate (CSG-452 hydrate) 是一种有效的,选择性的 SGLT2抑制剂,IC50为 2.9 nM,对人、大鼠和小鼠 SGLT2的Ki 分别为 2.9 nM,14.9 nM 和 6.4 nM。Tofogliflozin hydrate 对肾小管细胞中高葡萄糖诱导的ROS 生成具有部分抑制作用。
T68174 Sergliflozin A

SGLT GPCR/G Protein
Sergliflozin A 是一种选择型SGLT2抑制剂,以剂量依赖性方式诱导糖尿。可降低高血糖。
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。
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。
T28757 Sergliflozin etabonate

GW-869682,GW-869682X,KGT-1251,GW869682X,GW869682,KGT1251

SGLT GPCR/G Protein
Sergliflozin etabonate (KGT-1251) 是一种 SGLT-2 抑制剂,可用于 2 型糖尿病和肥胖症的研究。
T15656 KGA-2727

SGLT GPCR/G Protein
KGA-2727是选择性,高亲和力和口服有效的 SGLT1抑制剂,对人和大鼠 SGLT1的 Ki 分别为 97.4 nM 和 43.5 nM,对 SGLT1的选择性比人SGLT2 高 140 倍 ,大鼠SGLT2高390 倍。KGA-2727具有抗糖尿病活性。
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。
T15244 Ertugliflozin L-pyroglutamic acid

埃格列净,PF-04971729 L-pyroglutamic acid

Others; SGLT GPCR/G Protein; Others
Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) 是一种特异性和口服活性的 hSGLT2 抑制剂,IC50 为 0.877 nM。 Ertugliflozin L-pyroglutamic acid 可用于治疗 2 型糖尿病的研究。
T1766 Empagliflozin

BI 10773,恩格列净

SGLT GPCR/G Protein
Empagliflozin (BI 10773) 是一种 SGLT-2 抑制剂 (IC50=3.1 nM),具有有效的和选择性,对 SGLT-1/4/5/6 的选择性高 300 倍以上。Empagliflozin 可用于治疗二型糖尿病。
T15505 HSK0935

HSK 0935,HSK-0935

SGLT GPCR/G Protein
HSK0935 is a highly selective and orally available SGLT2 inhibitor (IC50: 1.3 nM). It has antihyperglycemic activities.
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).
T21399 Luseogliflozin

TS71,TS-071,TS 71,TS071,TS-71,TS 071

Luseogliflozin, a potent and competitive inhibitor of sodium-dependent glucose cotransporter 2 (SGLT2), competitively inhibits human SGLT2-mediated glucose uptake with a Ki value of 1.10 nM.
T32058 Henagliflozin

SHR3824,SHR 3824,SHR-3824

Henagliflozin (SHR3824) is an effective, oral, and selective SGLT2 inhibitor that effectively inhibits human SGLT2 in vitro, but has very weak inhibitory effects on human SGLT1.
T13179 Tofogliflozin

CSG452

Others Others
Tofogliflozin is a highly specific inhibitor of sodium/glucose cotransporter 2 (SGLT2) (Kis: 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2. IC50s: 2.9/14.9/6.4 nM (human/rat/mouse SGLT2)).
T15752 Licogliflozin

LIK066

SGLT GPCR/G Protein
Licogliflozin (LIK066) 是钠-葡萄糖协同转运蛋白 (SGLT1和SGLT2) 的有效抑制剂。
T3450 LX4211 N-4 Intermediate 9

索格列净中间体9,Sotagliflozin Intermediate 9

LX4211 N-4 Intermediate 9 是 Sotagliflozin 的中间体,Sotagliflozin 是一种口服生物可利用的 SGLT1 和 SGLT2 抑制剂。
T11667 Ipragliflozin (L-Proline)

Ipragliflozin L-Proline

Others Others
Ipragliflozin is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
T10669 Canagliflozin-d4

Canagliflozin D4

Others Others
Canagliflozin D4 is a deuterium-labeled Canagliflozin. Canagliflozin is an SGLT2 inhibitor.
T39966 SGLT1/2-IN-2

SGLT1/2-IN-2

SGLT1/2-IN-2 is a chemical compound with robust dual inhibitory properties, exhibiting potent activities against SGLT1 (IC50 = 96 nM) and SGLT2 (IC50 = 1.3 nM).
T15797 LX2761

Others Others
LX2761 is a chemically stable and effective inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 (IC50s: 2.2 nM and 2.7nM for hSGLT1 and hSGLT2). However, it shows specific SGLT1 inhibition in the gastrointestinal (GI) tract.
T72143 Velagliflozin proline hydrate

Velagliflozin proline hydrate 是 Velagliflozin 的临床形式。Velagliflozin 是一种可口服的钠-葡萄糖协同转运蛋白 2 (SGLT2) 抑制剂,具有抗糖尿病的活性。 特别是,Velagliflozin 减少肾葡萄糖重吸收,促进葡萄糖尿,从而降低血糖和胰岛素浓度。
T30534 BMS-639432

BMS-639432 is a potent sodium-glucose cotransporter type II (SGLT2) inhibitor.
T35619 Dapagliflozin-3-O-β-D-Glucuronide

Dapagliflozin-3-O-β-D-glucuronide is a metabolite of dapagliflozin . Dapagliflozin is a first generation selective sodium glucose cotransporter (SGLT) 2 inhibitor that blocks glucose transport.[1] Dapagliflozin is metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A9 to dapagliflozin-3-O-β-D-glucuronide, which is 2,600-fold less potent than the parent compound with regard to SGLT2 inhibition.[2]
T62830 SGLT1/2-IN-1

SGLT1/2-IN-1 是一种 SGLT1/SGLT2 双重抑制剂.
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).
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...
T10958 Dapagliflozin-d5

BMS-512148 D5

Others Others
Dapagliflozin D5 (BMS-512148 D5) is deuterated Dapagliflozin. Dapagliflozin is a competitive SGLT2 inhibitor.
T34767 TA-1887

TA 1887,TA1887

TA-1887 is a new type of selective inhibitor of sglt2 for the treatment of type 2 diabetes. It has a significant hypoglycemic effect in KK (HF-KK) mice fed a high-fat diet. TA-1887 has good pharmacokinetic characteristics and significantly increases UGE
T12892 SGL5213

SGLT GPCR/G Protein
SGL5213 is an oral active and low-absorbable inhibitor of sodium-dependent glucose cotransporter 1 (SGLT1)(hSGLT1 and hSGLT2 with IC50 values of 29 nM and 20 nM , respectively),and has potential to treat type 2 diabetes.
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).

化合物

T-1095
Cat.No: T9590
Synonym:
Target: SGLT, transporter
Ipragliflozin
Cat.No: T2385
Synonym: 伊格列净,ASP1941
Target: SGLT
Ertugliflozin
Cat.No: T4999
Synonym: 埃格列净,MK-8835,PF-04971729
Target: SGLT
Canagliflozin
Cat.No: T1782
Synonym: 卡格列净,JNJ 24831754ZAE,JNJ 28431754AAA,TA 7284,JNJ 28431754
Target: SGLT
Remogliflozin etabonate
Cat.No: T34286
Synonym: GSK189075,GSK 189075,GSK-189075A,GSK189075A,GSK-189075,GSK 189075A
Target: SGLT
Dapagliflozin
Cat.No: T2389
Synonym: 达格列净,BMS-512148
Target: SGLT, HIF
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
O-Desethyl Dapagliflozin
Cat.No: T67849
Synonym: Empagliflozin-4
Target: SGLT
Bexagliflozin
Cat.No: T7217
Synonym: THR-1442,EGT1442,EGT0001442
Target: SGLT
Tofogliflozin (hydrate)
Cat.No: T5016
Synonym: 托格列净,Tofogliflozin hydrate,CSG-452 hydrate
Target: SGLT, Reactive Oxygen Species, ROS
Sergliflozin A
Cat.No: T68174
Synonym:
Target: SGLT
Mizagliflozin
Cat.No: T16083
Synonym: GSK-1614235 free base,KGA-3235 free base,DSP-3235 free base
Target: SGLT
Sotagliflozin
Cat.No: T3547
Synonym: LX-4211,LP-802034
Target: SGLT
Sergliflozin etabonate
Cat.No: T28757
Synonym: GW-869682,GW-869682X,KGT-1251,GW869682X,GW869682,KGT1251
Target: SGLT
KGA-2727
Cat.No: T15656
Synonym:
Target: SGLT
Canagliflozin hemihydrate
Cat.No: T1782L
Synonym: JNJ28431754,TA 7284,TA7284,TA-7284,JNJ 28431754,JNJ-28431754
Target: SGLT
Ertugliflozin L-pyroglutamic acid
Cat.No: T15244
Synonym: 埃格列净,PF-04971729 L-pyroglutamic acid
Target: Others, SGLT
Empagliflozin
Cat.No: T1766
Synonym: BI 10773,恩格列净
Target: SGLT
HSK0935
Cat.No: T15505
Synonym: HSK 0935,HSK-0935
Target: SGLT
Luseogliflozin hydrate
Cat.No: T38539
Synonym: 鲁格列净水合物,TS 071 hydrate
Target:
Luseogliflozin
Cat.No: T21399
Synonym: TS71,TS-071,TS 71,TS071,TS-71,TS 071
Target:
Henagliflozin
Cat.No: T32058
Synonym: SHR3824,SHR 3824,SHR-3824
Target:
Tofogliflozin
Cat.No: T13179
Synonym: CSG452
Target: Others
Licogliflozin
Cat.No: T15752
Synonym: LIK066
Target: SGLT
LX4211 N-4 Intermediate 9
Cat.No: T3450
Synonym: 索格列净中间体9,Sotagliflozin Intermediate 9
Target:
Ipragliflozin (L-Proline)
Cat.No: T11667
Synonym: Ipragliflozin L-Proline
Target: Others
Canagliflozin-d4
Cat.No: T10669
Synonym: Canagliflozin D4
Target: Others
SGLT1/2-IN-2
Cat.No: T39966
Synonym: SGLT1/2-IN-2
Target:
LX2761
Cat.No: T15797
Synonym:
Target: Others
Velagliflozin proline hydrate
Cat.No: T72143
Synonym:
Target:
BMS-639432
Cat.No: T30534
Synonym:
Target:
Dapagliflozin-3-O-β-D-Glucuronide
Cat.No: T35619
Synonym:
Target:
SGLT1/2-IN-1
Cat.No: T62830
Synonym:
Target:
Remogliflozin
Cat.No: T24708
Synonym: GSK189074,Remogliflozin A,GSK-189074,GSK 189074
Target:
YM-543 choline
Cat.No: T70390
Synonym:
Target:
Dapagliflozin-d5
Cat.No: T10958
Synonym: BMS-512148 D5
Target: Others
TA-1887
Cat.No: T34767
Synonym: TA 1887,TA1887
Target:
SGL5213
Cat.No: T12892
Synonym:
Target: SGLT
SGLT inhibitor-1
Cat.No: T12893
Synonym:
Target: SGLT
Cat. No. Product Name Target Signaling Pathways
TN1847 Kushenol X

苦参醇X

Others Others
Kushenol X exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).
TN1841 Kushenol A

苦参新醇 A,Leachianone E

cAMP GPCR/G Protein
Kushenol A is a kind of Adenosine 3', 5'-cyclic monophosphate(cAMP)phosphodiesterase inhibitiors, it shows selective alpha-glucosidase inhibitory activity. Kushenol A and kushenol C exhibit inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).
T2922 Phlorizin

Floridzin,根皮甙,根皮苷,NSC 2833,Phloridzin

ATPase; SGLT GPCR/G Protein; Membrane transporter/Ion channel
Phlorizin (Phloridzin) 是非选择性的SGLT 抑制剂,也是Na+/K+-ATPase 抑制剂,对于hSGLT1和hSGLT2的Ki 值分别为 300 和 39 nM。
TN1842 Kushenol I

GABA Receptor; Antifection Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Kushenol I is a GABAA receptor modulator, it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).Kushenol I is shown to be active against the plant pathogenic fungus Cladosporium cucumerinum.
TN4399 Kushenol C

SGLT; NF-κB; ROS; BACE; Antifection GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB
Kushenol C is a good 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenger, and it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2). Kushenol C shows antimicrobial activity against Staphylococcus aureus and Streptococcus mutan

天然产物

Kushenol X
Cat.No: TN1847
Synonym: 苦参醇X
Target: Others
Kushenol A
Cat.No: TN1841
Synonym: 苦参新醇 A,Leachianone E
Target: cAMP
Phlorizin
Cat.No: T2922
Synonym: Floridzin,根皮甙,根皮苷,NSC 2833,Phloridzin
Target: ATPase, SGLT
Kushenol I
Cat.No: TN1842
Synonym:
Target: GABA Receptor, Antifection
Kushenol C
Cat.No: TN4399
Synonym:
Target: SGLT, NF-κB, ROS, BACE, Antifection
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