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Search Results for " gpr40 agonist "

41

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
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.
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).
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。
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。
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。
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。
T27937	LY2881835 LY 2881835,LY-2881835
	LY2881835 is a potent and selective GPR40 agonist.
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。
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。
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。
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。
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。
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.
T26609	AM-5262 AM 5262,AM5262
	AM-5262 is a potent GPR40 Full Agonist with improved rat PK profile and general selectivity profile.
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.
T23712	AM-6226 AM 6226
	AM-6226 is a potent and orally bioavailable GPR40 full agonist.
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).
T68243	AS1975063
	AS1975063 is a GPR40 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.
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。
T70373	AS2575959
	AS2575959 is a novel GPR40 agonist, exhibiting glucose metabolism improvement and synergistic effect with sitagliptin on insulin and incretin secretion.
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。
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.
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.
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
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
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.
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
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.
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.
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。
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。
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。
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...
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...
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 Agonist 2

Cat.No: T10507

Target: GPR

GPR40 agonist 1

Cat.No: T11459

Target: Others

GPR40 agonist 4

Cat.No: T15267

Target: Others

GPR40 agonist 6

Cat.No: T61055

GPR40 agonist 5

Cat.No: T62542

GPR40/FFAR1 modulator 1

Cat.No: T11458

Target: GPR

Cat.No: T15810

Target: GPR

Cat.No: T2351

Synonym: TAK875

Target: GPR

Cat.No: T27937

Synonym: LY 2881835,LY-2881835

Fezagepras sodium

Cat.No: T12375

Synonym: Setogepram sodium salt,PBI-4050 sodium salt

Target: GPR

Cat.No: T22967

Synonym: MEDICA 16

Target: GPR, Others, ATP Citrate Lyase

AMG 837 calcium hydrate

Cat.No: TQ0020

Target: GPR

Cat.No: T1781

Synonym: GW 9508

Target: GPR, Potassium Channel

Cat.No: T12883

Synonym: PBI-4050,3-戊基苯乙酸,Setogepram

Target: GPR

Cat.No: T60184

Target: GPR, PPAR

Cat.No: T17177

Synonym: TUG424

Target: Others

Cat.No: T15448

Target: GPR

Cat.No: T26609

Synonym: AM 5262,AM5262

Cat.No: T11583

Target: Others

Cat.No: T23712

Synonym: AM 6226

Cat.No: TQ0241

Target: GPR

Cat.No: T68243

Cat.No: T14202

Target: GPR

TAK-875 Hemihydrate

Cat.No: T2351L

Synonym: TAK-875,Fasiglifam

Target: GPR

Cat.No: T70373

Cat.No: T63404

Cat.No: T14200

Target: GPR

Cat.No: T13550

Target: Others

Cat.No: T27938

Synonym: LY 2922083,LY-2922083

AMG 837 sodium salt

Cat.No: T14215

Target: Others

Cat.No: T26868

Synonym: BMS 986118

Cat.No: T69953

Cat.No: T14216

Target: Others

Cat.No: T39140

Cat.No: T70468

AMG 837 hemicalcium

Cat.No: T62848

Cat.No: T63202

Cat.No: T73434

Cat.No: T36634

Cat.No: T68356

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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