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Search Results for " t2dm "

Targets Recommended: GPR

34

抑制剂 & 化合物

2

天然产物

1

化合物库

3

重组蛋白

1

同位素标记化合物

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Cat. No.	Product Name
L2540	肠道微生物代谢化合物库		614 compounds
	614 种肠道微生物代谢物的集合，可以用于高通量和高内涵筛选；

化合物库

肠道微生物代谢化合物库

Cat.No: L2540

Compounds: 614

Cat. No.	Product Name	Target	Signaling Pathways
T2701	GSK1292263	GPR	Endocrinology/Hormones; GPCR/G Protein
	GSK1292263 是口服具有活性的 GPR119 激动剂，对人和大鼠 GPR119的pEC50分别为 6.9 和 6.7，它可用于研究 2 型糖尿病 (T2DM) 。
T9022	AZD9977 AZD 9977	Glucocorticoid Receptor	Endocrinology/Hormones
	AZD9977 是一种选择性的，有效的，具有口服活性的盐皮质激素受体 (MR) 调节剂，可用于研究心力衰竭和慢性肾病。
T15432	GSK256073	GPR; Others	Endocrinology/Hormones; GPCR/G Protein; Others
	GSK256073 是一种口服有活性的GPR109A 选择性激动剂，也是一种持久的人HCA2激动剂(pEC50:7.5) 。它能够减少脂降解，而显著改善葡萄糖稳态，对 2 型糖尿病和血脂异常具有潜在的研究价值。
T12710	Retagliptin Phosphate SP 2086,瑞格列汀磷酸盐	Proteasome; DPP-4	Proteases/Proteasome; Ubiquitination
	Retagliptin Phosphate (SP 2086) 是一种选择性、竞争性、口服活性的二肽基肽酶 4 (DPP-4) 抑制剂。Retagliptin phosphate 能够用于 2 型糖尿病 (T2DM) 的研究。
T2371	Emapunil AC-5216,XBD-173	Others	Others
	Emapunil (XBD-173) 是一种选择性的、口服有效的TSPO(一种线粒体苯二氮受体) 的配体。在多种动物模型中，它显示出抗焦虑和抗抑郁特性。
T8780	AMG131 INT-131,AMG-131,CHS 131	PPAR	DNA Damage/DNA Repair; Metabolism
	AMG131 (CHS 131) 是一种新型非噻唑烷二酮(TZD) 选择性过氧化物酶体增殖物激活受体 (PPAR) γ 调节剂，可用于治疗 2 型糖尿病。
TP1469	Lixisenatide acetate (320367-13-3 free base) Lixisenatide acetate	Glucagon Receptor	GPCR/G Protein
	Lixisenatide acetate 是一种胰高血糖素样肽 1 受体的激动剂，可用于研究 2 型糖尿病。
TP1796	Albiglutide TFA (782500-75-8 free base) Albiglutide TFA	Glucagon Receptor	GPCR/G Protein
	Albiglutide TFA (782500-75-8 free base) (Albiglutide TFA) 是一种长效 GLP-1 受体激动剂，用于治疗 2 型糖尿病 (T2DM)。
T27439	GS-9667 CVT-3619,CVT 3619	Adenosine Receptor	GPCR/G Protein; Neuroscience
	GS-9667是一种A（1）腺苷受体（AR）的选择性部分激动剂，通过降低游离脂肪酸（FFA）可有效治疗2型糖尿病（T2DM）和血脂异常。
T77781	Lotiglipron PF-07081532	Glucagon Receptor	GPCR/G Protein
	Lotiglipron (PF-07081532) 是一种具有口服活性和有效性的 GLP-1R 激动剂，能够降低血糖和体重，可用于研究 2 型糖尿病 (T2DM) 和过度肥胖。
T27841	Lobeglitazone Sulfate CKD501 Sulfate,CKD501,CKD-501 Sulfate,CKD 501 Sulfate,CKD 501,CKD-501,Lobeglitazone Sulfate. trade name Duvie, Chong Kun Dang	NOD	Immunology/Inflammation; NF-κB
	Lobeglitazone Sulfate（CKD-501 Sulfate）是一种新型噻唑烷二酮,具有抗炎活性，抑制LPS诱导的NLRP3炎症小体活化和肝脏炎症，可用于研究 2 型糖尿病 (T2DM)。
T67898	α-Glucosidase-IN-22	Glucosidase	Metabolism
	α-Glucosidase-IN-22是一种α-葡萄糖苷酶选择性抑制剂（IC50=0.64 μM）。α-Glucosidase-IN-22有抗糖尿病的活性，在2型糖尿病(T2DM)研究中具有潜力。
T16486	Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD PF-05231023	FGFR; PROTAC Linker	Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors
	Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD (PF-05231023) 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 的合成分子。
T6237	Trelagliptin SYR-472,曲格列汀	Proteasome; DPP-4	Proteases/Proteasome; Ubiquitination
	Trelagliptin (SYR-472) 是一种有效的，具有口服活性的DPP-4抑制剂，IC50=4 nM。它可以改善体内血糖控制，能够用于2 型糖尿病 (T2DM) 的研究。
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。
T2296	Trelagliptin succinate 曲格列汀琥珀酸盐,琥珀酸曲格列汀,SYR-472 succinate,SYR472	Proteasome; DPP-4	Proteases/Proteasome; Ubiquitination
	Trelagliptin succinate (SYR-472 succinate) 是一种有效的，具有口服活性的DPP-4抑制剂，IC50=4 nM。它可以改善体内血糖控制，能够用于2 型糖尿病(T2DM) 的研究。
T15810	LY2922470	GPR	Endocrinology/Hormones; GPCR/G Protein
	LY2922470 是选择性口服有效的GPR40激动剂，作用于人 GPR40、小鼠 GPR40、大鼠 GPR40 的EC50值分别为 7 nM、1 nM、3 nM。它可降低血糖水平，同时显著增加胰岛素和 GLP-1，有潜力用于 2 型糖尿病的研究。
T13022L	SSTR5 antagonist 2 TFA	Others	Others
	SSTR5 antagonist 2 TFA is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5), with potential to treat type 2 diabetes mellitus (T2DM).
T11416	Glucagon receptor antagonists-5	Others	Others
	Glucagon receptor antagonists-5 is an orally bioavailable indazole-based glucagon receptor antagonist (Ki: 32 nM). It has potential for the treatment of type 2 diabetes mellitus (T2DM).
T13022	SSTR5 antagonist 2	Others	Others
	SSTR5 antagonist 2 is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5),with potential to treat type 2 diabetes mellitus (T2DM).
T78313	Fazpilodemab BFKB8488A	FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Fazpilodemab (BFKB8488A) 是靶向 FGFR1c 和 Klothoβ 的激动性人源化双特异性抗体，适用于T2DM或NAFLD的研究。
T38539	Luseogliflozin hydrate 鲁格列净水合物,TS 071 hydrate	Others	Others
	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).
T78731	α-Glucosidase-IN-26	Glucosidase	Metabolism
	α-Glucosidase-IN-26（化合物 7i）是一种有效的α-glucosidase抑制剂，其半抑制浓度（IC50）为4.63 µM，适用于2型糖尿病（T2DM）的研究。
T78703	PTP1B/AKR1B1-IN-2	Phosphatase	Metabolism
	PTP1B/AKR1B1-IN-2（化合物7f）是一种双重PTP1B/AKR1B1抑制剂，具有IC50：3.2和2.1 μM，Ki：4.0和0.9μM。该化合物作为胰岛素模拟剂，能够改善小鼠C2C12肌母细胞的葡萄糖摄取，并可用于2型糖尿病（T2DM）的研究。
T62985	Cofrogliptin	Others	Others
	Cofrogliptin (HSK7653) (compound 2) 是一种四氢吡喃衍生物，是一种口服具有活力的 DPP-4 抑制剂，具有长效降糖作用。Cofrogliptin (compound 2) 具有潜力进行 2 型糖尿病 (T2DM) 的研究。
TP1340	Lixisenatide
	Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM).It is an injectable diabetes medicine that helps control blood sugar levels.
T60203	INCB13739	Others	Others
	INCB13739是一种具有口服活性、高效、选择性及组织特异性的11β-HSD1抑制剂，对11β-HSD1酶的IC50为3.2 nM，对11β-HSD1 PBMC的IC50为1.1 nM。适用于2型糖尿病(T2DM)和肥胖的研究。
T40349	DS45500853	Others	Others
	DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM), exhibiting an IC50 of 0.80 μM. This compound holds potential for research pertaining to metabolic disorders, particularly type 2 diabetes mellitus (T2DM).
T60759	DS20362725	Others	Others
	DS20362725 是可用于代谢紊乱研究，如二型糖尿病的雌激素相关受体 α (ERRα) 激动剂。DS20362725 抑制受体相互作用蛋白 140 (RIP140) 辅助抑制肽 (10 nM) 和 GST-ERRα 配体结合结构域 (LBD; 1.2 μM) 之间的结合的 IC50值为 0.6 μM。
T78881	α-Glucosidase-IN-36	Glucosidase	Metabolism
	α-Glucosidase-IN-36（compound 5g）作为一种α-glucosidase抑制剂，表现出有效的抑制活性，其IC50值为6.69 ± 0.18 μM，Ki值为1.65 μM，Kis值为4.54 μM。该化合物通过与α-glucosidase的活性位点结合及可能改变其二级结构来执行其抑制功能。α-Glucosidase-IN-36在2型糖尿病（T2DM）的研究中有应用潜力。
T79358	PF-07247685	Endogenous Metabolite	Metabolism
	PF-07247685是一种BCKDC激酶(BDK)抑制剂，具有较强的活性(EC50=2.2 nM)。该化合物能有效稳定BDK与BCKDH E2核心亚基之间的相互作用，并阻断E1亚基的磷酸化过程。BCKDH的活性受到BDK介导的磷酸化调控，从而控制支链氨基酸(BCAA)降解的关键步骤。BCAA的代谢失调与心力衰竭(HF)、2型糖尿病(T2DM)、非酒精性脂肪肝病(NAFLD)及肥胖等多种疾病相关联，尤其在心脏代谢疾病中表现明显。PF-07247685在小鼠模型中对心脏代谢终点产生改善效果，并提升了葡萄糖耐量。
T70391	AMG151 HCl	Others	Others
	ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesse...
T79357	PF-07238025	Endogenous Metabolite	Metabolism
	PF-07238025是一种BCKDC激酶(BDK)抑制剂，具有EC50值为19 nM。它通过稳定BDK和BCKDH复合体中的E2亚基相互作用，阻碍E1亚基的磷酸化过程，从而抑制了BCKDH的活性。由于BDK的磷酸化作用是控制支链氨基酸(BCAA)降解过程中的限速步骤，PF-07238025的作用与包括心力衰竭(HF)、2型糖尿病(T2DM)、非酒精性脂肪肝病(NAFLD)及肥胖在内的多种代谢性疾病的发病机制相关。研究显示PF-07238025能在小鼠体内改善心脏代谢指标并提升葡萄糖耐量。
T78702	PTP1B/AKR1B1-IN-1	Phosphatase	Metabolism
	PTP1B/AKR1B1-IN-1是一种针对PTP1B和AKR1B1的双重抑制剂，其IC50值分别为0.06 μM和4.3 μM。该化合物也能抑制TC-PTP，IC50为9 μM。在小鼠成肌细胞中，PTP1B/AKR1B1-IN-1作为胰岛素模拟剂使用，并能减少AKR1B1依赖的山梨醇积累，有助于抑制2型糖尿病的发展并控制血糖水平。

化合物

Cat.No: T2701

Target: GPR

Cat.No: T9022

Synonym: AZD 9977

Target: Glucocorticoid Receptor

Cat.No: T15432

Target: GPR, Others

Retagliptin Phosphate

Cat.No: T12710

Synonym: SP 2086,瑞格列汀磷酸盐

Target: Proteasome, DPP-4

Cat.No: T2371

Synonym: AC-5216,XBD-173

Target: Others

Cat.No: T8780

Synonym: INT-131,AMG-131,CHS 131

Target: PPAR

Lixisenatide acetate (320367-13-3 free base)

Cat.No: TP1469

Synonym: Lixisenatide acetate

Target: Glucagon Receptor

Albiglutide TFA (782500-75-8 free base)

Cat.No: TP1796

Synonym: Albiglutide TFA

Target: Glucagon Receptor

Cat.No: T27439

Synonym: CVT-3619,CVT 3619

Target: Adenosine Receptor

Cat.No: T77781

Synonym: PF-07081532

Target: Glucagon Receptor

Lobeglitazone Sulfate

Cat.No: T27841

Synonym: CKD501 Sulfate,CKD501,CKD-501 Sulfate,CKD 501 Sulfate,CKD 501,CKD-501,Lobeglitazone Sulfate. trade name Duvie, Chong Kun Dang

Target: NOD

α-Glucosidase-IN-22

Cat.No: T67898

Target: Glucosidase

Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD

Cat.No: T16486

Synonym: PF-05231023

Target: FGFR, PROTAC Linker

Cat.No: T6237

Synonym: SYR-472,曲格列汀

Target: Proteasome, DPP-4

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

Trelagliptin succinate

Cat.No: T2296

Synonym: 曲格列汀琥珀酸盐,琥珀酸曲格列汀,SYR-472 succinate,SYR472

Target: Proteasome, DPP-4

Cat.No: T15810

Target: GPR

SSTR5 antagonist 2 TFA

Cat.No: T13022L

Target: Others

Glucagon receptor antagonists-5

Cat.No: T11416

Target: Others

SSTR5 antagonist 2

Cat.No: T13022

Target: Others

Cat.No: T78313

Synonym: BFKB8488A

Target: FGFR

Luseogliflozin hydrate

Cat.No: T38539

Synonym: 鲁格列净水合物,TS 071 hydrate

Target: Others

α-Glucosidase-IN-26

Cat.No: T78731

Target: Glucosidase

PTP1B/AKR1B1-IN-2

Cat.No: T78703

Target: Phosphatase

Cat.No: T62985

Target: Others

Cat.No: TP1340

Cat.No: T60203

Target: Others

Cat.No: T40349

Target: Others

Cat.No: T60759

Target: Others

α-Glucosidase-IN-36

Cat.No: T78881

Target: Glucosidase

Cat.No: T79358

Target: Endogenous Metabolite

Cat.No: T70391

Target: Others

Cat.No: T79357

Target: Endogenous Metabolite

PTP1B/AKR1B1-IN-1

Cat.No: T78702

Target: Phosphatase

Cat. No.	Product Name	Target	Signaling Pathways
T1286	Vincamine Angiopac,Oxybral,Devincan,Novicet,Equipur,长春胺,Perval	GPR; Others	Endocrinology/Hormones; GPCR/G Protein; Others
	Vincamine (Perval) 是从长春花中提取的单萜类吲哚生物碱，可作为外周血管扩张剂，对脑微血管循环有选择性的血管调节作用。它可改善体内葡萄糖稳态，对 2 型糖尿病具有研究潜力。它是GPR40激动剂，通过改善 β 细胞功能障碍和促进葡萄糖刺激型胰岛素分泌发挥 β 细胞保护作用。
T3863	Chikusetsusaponin IVa 竹节参皂苷IVa,Calenduloside F,竹节人参皂苷 IVA	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	Chikusetsusaponin IVa (Calenduloside F) 是一种三萜皂苷中主要的活性成分，是一种蛋白激酶的激活剂，对血栓及一些代谢性疾病具有抵抗作用。

天然产物

Cat.No: T1286

Synonym: Angiopac,Oxybral,Devincan,Novicet,Equipur,长春胺,Perval

Target: GPR, Others

Chikusetsusaponin IVa

Cat.No: T3863

Synonym: 竹节参皂苷IVa,Calenduloside F,竹节人参皂苷 IVA

Target: AMPK

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPK-00678	CALCA/CGRP Protein, Mouse, Recombinant (hFc) CGRP,Katacalcin,PDN-21,CGRP-I,CGRP1,Calcitonin 1,Calcitonin,...	Mouse	HEK293 Cells
	Specific fragments of methylation changes in the target gene (Calca) were identified by IGV analysis. CGRP was applied to compare the effects on ASCs-T2DM morphology via phalloidin staining, proliferation through CCK-8 assay, and osteogenic differentiation with osteogenic staining, qPCR, and repair of calvarial defect. Furthermore, 5-azacytidine (5-az) was used to intervene ASCs-T2DM to verify the relationship between the methylation level of the target fragment and expression of Calca.
TMPY-04478	IP6K1/IHPK1 Protein, Human, Recombinant (His & GST) inositol hexakisphosphate kinase 1,IHPK1,PiUS	Human	Baculovirus Insect Cells
	IP6K1 (Inositol Hexakisphosphate Kinase 1) is a Protein Coding gene. 2 alternatively spliced human isoforms have been reported. IHPK1 is an inositol hexaphosphate kinase (IHPK) protein that belongs to the inositol phosphokinase (IPK) family. IHPK proteins are likely responsible for the conversion of inositol hexakisphosphate (InsP6) to diphosphoinositol pentakisphosphate (InsP7/PP-InsP5). IHPK1 may also convert 1,3,4,5,6-pentakisphosphate (InsP5) to PP-InsP4 and affect the growth-suppressive and...
TMPJ-00014	Resistin Protein, Human, Recombinant (His) Resistin,C/EBP-epsilon-regulated myeloid-specific secreted c...	Human	E. coli
	Resistin known as adipose tissue-specific secretory factor (ADSF) or C/EBP-epsilon-regulated myeloid-specific secreted cysteine-rich protein (XCP1) that seems to suppress insulin ability to stimulate glucose uptake into adipose cells. The length of the resistin pre-peptide in human is 108 amino acid residues and in the mouse and rat it is 114 aa; the molecular weight is ~12.5 kDa. Resistin is a cytokine whose physiologic role has been the subject of much controversy regarding its involvement wit...

重组蛋白

CALCA/CGRP Protein, Mouse, Recombinant (hFc)

Cat.No: TMPK-00678

Species: Mouse

Expression System: HEK293 Cells

IP6K1/IHPK1 Protein, Human, Recombinant (His & GST)

Cat.No: TMPY-04478

Species: Human

Expression System: Baculovirus Insect Cells

Resistin Protein, Human, Recombinant (His)

Cat.No: TMPJ-00014

Species: Human

Expression System: E. coli

Cat. No.	Product Name	Target	Signaling Pathways
TMIH-0583	Trelagliptin-13C-d3
	Trelagliptin-13C-d3 是 Trelagliptin 的 13C 和氘代化合物。Trelagliptin 的 CAS 号为 865759-25-7。Trelagliptin 是一种有效的，具有口服活性的DPP-4抑制剂，IC50=4 nM。它可以改善体内血糖控制，能够用于2 型糖尿病 (T2DM) 的研究。

同位素标记化合物

Trelagliptin-13C-d3

Cat.No: TMIH-0583

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