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抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11458	GPR40/FFAR1 modulator 1	GPR	Endocrinology/Hormones; GPCR/G Protein
	GPR40/FFAR1 modulator 1是一种针对Gq偶联的游离脂肪酸受体1 (GPR40/FFAR1) 的激动剂以及异构调节剂。
T11459	GPR40 agonist 1	Others	Others
	GPR40 agonist 1 is an effective new GPR40 agonist (EC50s: 17 nM and 2 nM for rGPR40 and hGPR40).
T15267	GPR40 agonist 4	Others	Others
	GPR40 agonist 4 is a potent free fatty acid agonist of receptor 1 (pEC50: 7.54).
T10507	GPR40 Agonist 2	GPR	Endocrinology/Hormones; GPCR/G Protein
	GPR40 Agonist 2 is a GPR40 agonist. It can be used in the research of diabetes.
T11457	GPR40 Activator 2	Others	Others
	GPR40 Activator 2 is a highly effective activator of the GPR40 receptor.
T11456	GPR40 Activator 1	Others	Others
	GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.
T62542	GPR40 agonist 5
	GPR40 agonist 5 是一种口服具有活力的 GPR40 (G 蛋白偶联受体 40) 激动剂 (EC50: 47 nM)。GPR40 agonist 5 能够减少血糖水平，改善糖耐量。GPR40 agonist 5 对 2 型糖尿病小鼠的高血糖状态表现出充足的控制作用。
T61055	GPR40 agonist 6
	GPR40 agonist 6 (Compound 7a) 是游离脂肪酸受体 1的选择性激动剂（FFAR1或GPR40），其对于GPR40的EC50值为 0.058 μM。
TQ0020	AMG 837 calcium hydrate	GPR	Endocrinology/Hormones; GPCR/G Protein
	AMG 837 calcium hydrate 是口服有效的 GPR40/FFA1部分激动剂，抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合，pIC50为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。
T1781	GW9508 GW 9508	GPR; Potassium Channel	Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel
	GW 9508 是一种选择性 G 蛋白偶联受体FFA1(GPR40) 和GPR120激动剂。它是一种葡萄糖敏感性胰岛素促分泌剂和 ATP 敏感性钾通道开放剂，具有抗炎和抗动脉粥样硬化活性。
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。
T2351	Fasiglifam TAK875	GPR	Endocrinology/Hormones; GPCR/G Protein
	Fasiglifam (TAK875) 是一种可口服的选择性GPR40激动剂，EC50值为 72 nM。
T60184	TUG-499	GPR; PPAR	DNA Damage/DNA Repair; Endocrinology/Hormones; GPCR/G Protein; Metabolism
	TUG-499 是一种选择性游离脂肪酸受体 1 (FFAR1 或 GPR40)激动剂（EC50 ： 7.39）。TUG-499对 FFAR1 或 GPR40的亲和力超过相关受体 FFA2、FFA3 和核受体 PPARγ，以及其他不同的受体、离子通道和转运蛋白。TUG-499 可用于研究 2 型糖尿病。
T7127	DC260126	Apoptosis; GPR	Apoptosis; Endocrinology/Hormones; GPCR/G Protein
	DC260126 是一种 GPR40 (FFAR1)拮抗剂，对棕榈酸酯诱导的内质网应激和凋亡有保护作用。它剂量依赖性地抑制亚油酸、油酸、棕榈油酸和月桂酸刺激的 GPR40 介导的 Ca2+升高，IC50分别 6.28、5.96、7.07和4.58 μM。
T12375	Fezagepras sodium Setogepram sodium salt,PBI-4050 sodium salt	GPR	Endocrinology/Hormones; GPCR/G Protein
	Fezagepras sodium (Setogepram sodium salt) 是口服有效的 GPR40 激动剂及 GPR84 拮抗剂或反向激动剂。Fezagepras sodium 可以减轻肝，肾和胰腺纤维化。Fezagepras sodium 具有抗炎，抗增殖和抗纤维化作用。
T27937	LY2881835 LY 2881835,LY-2881835
	LY2881835 is a potent and selective GPR40 agonist.
T22967	MEDICA16 MEDICA 16	GPR; Others; ATP Citrate Lyase	Endocrinology/Hormones; GPCR/G Protein; Metabolism; Others
	MEDICA16 是 GPR40 的特异性激动剂以及 GPR120 的部分激动剂。 MEDICA16 是一种 ATP-柠檬酸裂解酶抑制剂，可显着降低腓肠肌中的细胞内 TG 含量，同时增加胰岛素敏感性。
T12883	Fezagepras PBI-4050,3-戊基苯乙酸,Setogepram	GPR	Endocrinology/Hormones; GPCR/G Protein
	Fezagepras (Setogepram) 是一种可口服的 GPR40激动剂和GPR84拮抗剂或反向激动剂。它减轻肾、肝和胰腺纤维化，具有抗纤维化、抗炎和抗增殖作用。
T17177	TUG-424 TUG424	Others	Others
	TUG-424 是一种有效且选择性的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂，EC50 为 32 nM。TUG-424 在 100 nM 处显著增加葡萄糖刺激的胰岛素分泌。TUG-424 可能有助于探索 FFA1 在糖尿病或肥胖等代谢性疾病中的作用。
T15448	GW-1100	GPR	Endocrinology/Hormones; GPCR/G Protein
	GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.
T14202	AM-4668	GPR	Endocrinology/Hormones; GPCR/G Protein
	AM-4668 is a type 2 diabetes GPR40 agonist. For GPR40, in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), the EC50s are 3.6 nM and 36 nM, respectively.
T11583	HWL-088	Others	Others
	HWL-088 is a potent free fatty acid receptor 1 (FFA1/GPR40) agonist. HWL-088 significantly improves glucose tolerance in normal and diabetic models.
T2351L	TAK-875 Hemihydrate TAK-875,Fasiglifam	GPR	Endocrinology/Hormones; GPCR/G Protein
	TAK-875 Hemihydrate (Fasiglifam) 是一种选择性 GPR40 激动剂，EC50 为 14 nM，比油酸强 400 倍。
TQ0241	TUG-770	GPR	Endocrinology/Hormones; GPCR/G Protein
	TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).
T26868	BMS-986118 BMS 986118
	BMS-986118 is a full agonist of GPR40, is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial a
T14200	AM-1638	GPR	Endocrinology/Hormones; GPCR/G Protein
	AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM).
T13550	AP5	Others	Others
	AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor.
T26609	AM-5262 AM 5262,AM5262
	AM-5262 is a potent GPR40 Full Agonist with improved rat PK profile and general selectivity profile.
T23712	AM-6226 AM 6226
	AM-6226 is a potent and orally bioavailable GPR40 full agonist.
T69953	MK-8666 Tris
	MK-8666 Tris is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 Tris has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.
T63404	Xelaglifam
	Xelaglifam 是 G 蛋白偶联受体 40 (GPR40) 的有效激动剂，表现出降血糖作用。
T68243	AS1975063
	AS1975063 is a GPR40 agonist.
T70373	AS2575959
	AS2575959 is a novel GPR40 agonist, exhibiting glucose metabolism improvement and synergistic effect with sitagliptin on insulin and incretin secretion.
T14215	AMG 837 sodium salt	Others	Others
	AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t
T14216	AMG 837	Others	Others
	AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. Overall, AMG 837 was both highly potent and selective in vitro. AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a sup
T27938	LY2922083 LY 2922083,LY-2922083
	LY2922083 is a Potent and Selective GPR40 agonist. LY2922083 demonstrates potent, efficacious and durable dose dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion.
T70468	MK-8666
	MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.
T63202	AP5 sodium
	AP5 sodium 是选择性的、有效的、口服具有活力的 GPR40 受体激动剂，对内源性配体 (AgoPAM) 表现出正向变构调节效果。AP5 sodium 在大鼠和人肌醇一磷酸 (IP1) 实验中作用于 GPR40 受体，他们的 EC50值分别为 0.49 nM 和 0.8 nM。AP5 sodium 表现出研究 II 型糖尿病的潜能。
T62848	AMG 837 hemicalcium
	AMG 837 hemicalcium 是一种有效的、口服具有活力的 GPR40/FFA1部分激动剂。AMG 837 hemicalcium 能够抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合 (pIC50: 8.13)。AMG 837 hemicalcium 能够提高啮齿动物的胰岛素分泌，减少葡萄糖水平。
T39140	SCO-267
	SCO-267 is a potent allosteric full agonist of the GPR40 receptor, making it a valuable tool in studying chronic diseases like diabetes.
T73434	BI-2081
	BI-2081是一种GPR40 (FFAR1)部分激动剂，具有EC50值为4 nM。该化合物能诱导葡萄糖依赖性胰岛素释放，并降低血浆中葡萄糖含量，适用于研究代谢疾病，尤其是2型糖尿病。
T68356	AM-3189
	AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavai...
T36634	ZQ 16
	Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 \|Zhang et al (2016) Discovery and characte...
T71251	DS-1558
	DS-1558 is a potent and orally available GPR40 agonist.DS-1558 was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF rats. DS-1558 significantly and dose-dependently improved hyperglycemia and increased insulin secretion during the oral glucose tolerance test in Zucker fatty rats, the model of insulin resistance and glucose intolerance. DS-1558 not only increased the glucose-stimulated insulin secretion by GLP-1 but also potentiated the maximum insulinog...
T35816	ZLY032
	ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic st...

化合物

GPR40/FFAR1 modulator 1

Cat.No: T11458

Target: GPR

GPR40 agonist 1

Cat.No: T11459

Target: Others

GPR40 agonist 4

Cat.No: T15267

Target: Others

GPR40 Agonist 2

Cat.No: T10507

Target: GPR

GPR40 Activator 2

Cat.No: T11457

Target: Others

GPR40 Activator 1

Cat.No: T11456

Target: Others

GPR40 agonist 5

Cat.No: T62542

GPR40 agonist 6

Cat.No: T61055

AMG 837 calcium hydrate

Cat.No: TQ0020

Target: GPR

Cat.No: T1781

Synonym: GW 9508

Target: GPR, Potassium Channel

Cat.No: T15810

Target: GPR

Cat.No: T2351

Synonym: TAK875

Target: GPR

Cat.No: T60184

Target: GPR, PPAR

Cat.No: T7127

Target: Apoptosis, GPR

Fezagepras sodium

Cat.No: T12375

Synonym: Setogepram sodium salt,PBI-4050 sodium salt

Target: GPR

Cat.No: T27937

Synonym: LY 2881835,LY-2881835

Cat.No: T22967

Synonym: MEDICA 16

Target: GPR, Others, ATP Citrate Lyase

Cat.No: T12883

Synonym: PBI-4050,3-戊基苯乙酸,Setogepram

Target: GPR

Cat.No: T17177

Synonym: TUG424

Target: Others

Cat.No: T15448

Target: GPR

Cat.No: T14202

Target: GPR

Cat.No: T11583

Target: Others

TAK-875 Hemihydrate

Cat.No: T2351L

Synonym: TAK-875,Fasiglifam

Target: GPR

Cat.No: TQ0241

Target: GPR

Cat.No: T26868

Synonym: BMS 986118

Cat.No: T14200

Target: GPR

Cat.No: T13550

Target: Others

Cat.No: T26609

Synonym: AM 5262,AM5262

Cat.No: T23712

Synonym: AM 6226

Cat.No: T69953

Cat.No: T63404

Cat.No: T68243

Cat.No: T70373

AMG 837 sodium salt

Cat.No: T14215

Target: Others

Cat.No: T14216

Target: Others

Cat.No: T27938

Synonym: LY 2922083,LY-2922083

Cat.No: T70468

Cat.No: T63202

AMG 837 hemicalcium

Cat.No: T62848

Cat.No: T39140

Cat.No: T73434

Cat.No: T68356

Cat.No: T36634

Cat.No: T71251

Cat.No: T35816

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。

天然产物

Cat.No: T1286

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

Target: GPR, Others

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