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Search Results for " free fatty acid receptor "

39

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8642	4-CMTB	GPR	Endocrinology/Hormones; GPCR/G Protein
	4-CMTB 是选择性的游离脂肪酸受体 2(FFA2/GPR43)的激动剂以及正变构调节剂 (pEC50=6.38)。
T7482	3-chloro-5-hydroxybenzoic Acid	GPR	Endocrinology/Hormones; GPCR/G Protein
	3-Chloro-5-hydroxybenzoic acid 是一种口服具有活力的乳酸受体GPR81选择性激动剂，对人 GPR81 的EC50为 16 μM。肥胖小鼠模型中，它表现出良好的体内脂肪分解作用。
T7796	TUG-1375	GPR	Endocrinology/Hormones; GPCR/G Protein
	TUG-1375 是游离脂肪酸受体 2 (FFA2/GPR43) 激动剂(pKi:6.69)。它对 FFA3，FFA4，PPARα，PPARγ，PPARδ，LXRα 或 LXRβ 无作用。
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。
T4312	GPR120 Agonist 2 GPR120 receptor agonist	GPR	Endocrinology/Hormones; GPCR/G Protein
	GPR120 Agonist 2 是一种选择性 GPR120激动剂。
T3433	TUG-891 TUG 891,TUG891	GPR	Endocrinology/Hormones; GPCR/G Protein
	TUG-891 是一种选择性的长链游离脂肪酸受体 4 (FFA4/GPR120) 的激动剂。
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。
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。
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。
T22027	AH-7614 AH 7614	GPR	Endocrinology/Hormones; GPCR/G Protein
	AH-7614 (AH 7614) 是一种选择性的游离脂肪酸受体 4(FFA4/GPR120) 拮抗剂，对人和大小鼠 FFA4 的pIC50值分别为 7.1、8.1 和 8.1。它能够阻断多不饱和 ω-6 脂肪酸亚油酸和 FFA4 激动剂的作用。
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。
T15413	GPR120 Agonist 3 GPR120-IN-1	GPR	Endocrinology/Hormones; GPCR/G Protein
	GPR120 Agonist 3 (GPR120-IN-1) 是一种有效的、选择性的 Gpr120激动剂，logEC50为 −7.62。
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。
T3171	GSK137647A GSK 137647	GPR	Endocrinology/Hormones; GPCR/G Protein
	GSK137647A (GSK 137647) 是一种选择性FFA4激动剂，作用于人类和大小鼠FFA4的pEC50分别为6.3、6.1和6.2。
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。
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。
T9437	1-methoxycyclopropanecarboxylic acid	GPR	Endocrinology/Hormones; GPCR/G Protein
	1-methoxycyclopropanecarboxylic acid 是游离脂肪酸受体 3 (FFAR3, human) 的激动剂。
T34967	TUG-469 TUG469,TUG 469	GPR	Endocrinology/Hormones; GPCR/G Protein
	TUG-469 是游离脂肪酸 1(FFA) 受体的激动剂。
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。
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。
TP1930L1	Spexin acetate(1370290-58-6 free base)	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	Spexin acetate(1370290-58-6 free base) 是一种有效的甘丙肽受体 2/3 (GAL2/GAL3) 激动剂（EC50 值分别为 45.7 和 112.2 nM）。对甘丙肽受体 1 没有显着的活性。抑制脂肪细胞对长链脂肪酸的摄取并减少饮食诱导的肥胖小鼠和大鼠的食物消耗。减少金鱼的 LH 分泌。在体内表现出抗焦虑作用。
T15267	GPR40 agonist 4	Others	Others
	GPR40 agonist 4 is a potent free fatty acid agonist of receptor 1 (pEC50: 7.54).
T25508	HUHS2002 HUHS 2002,HUHS-2002
	HUHS2002 is a free fatty acid derivative that works as a potentiator of GluA1 AMPA receptor responses and α7 ACh receptor responses.
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).
T34968	TUG-905
	TUG-905 is an agonist for free fatty acid receptor 4 (FFA4/GPR120), and TUG-905 has the potential to treat agitation.
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.
T26935	C108297 C-108297,C 108297
	C108297 is a glucocorticoid receptor modulator. C108297 prevents both diet-induced obesity and inflammation. C108297 decreased food and fructose intake and increased lipolysis in white adipose tissue (WAT) and free fatty acid levels in plasma, resulting i
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...
T27228	E-3030 free acid E-3030,E3030,E 3030
	E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr
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。
T38070	Arachidonic Acid-biotin
	Virtually all cellular arachidonic acid is esterified in membrane phospholipids where its presence is tightly regulated through multiple interconnected pathways. Free arachidonic acid is a transient, critical substrate for the biosynthesis of eicosanoid second messengers. Receptor-stimulated release, metabolism, and re-uptake of free arachidonate are all important aspects of cell signalling and inflammation. Arachidonic acid-biotin was designed to allow arachidonic acid to be detected in complex...
T71663	FFA3 agonist 1
	FFA3 agonist 1为一种FFA3（游离脂肪酸受体 3）激动剂，功能为通过激活FFA3以调节肠道微生物群的健康效应。
T69824	PSB-17365
	PSB-17365 is a potent GPR84 agonist. PSB-17365 exhibits EC50 values vs. GPR84 of 2.5nM in a cAMP accumulation assay, and 100nM in a β-arrestin 2 recruitment assay. No direct binding affinities are provided. PSB-17365 is selective for GPR84 compared to other free fatty acid receptors (FFAR1 and FFAR4). GPR84, a Gi protein-coupled receptor that is activated by medium-chain (hydroxy)fatty acids, appears to play an important role in inflammation, immunity, and cancer.
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.
T69953	MK-8666 Tris
	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.
T35791	Palmitic acid-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic ...
T37896	AZ 1729
	FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel...
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...
T83955	MOMBA
	MOMBA是一种针对人类自由脂肪酸2(hFFA2)工程化受体和设计药物激活的设计受体(DREADD)的选择性正交激动剂，对野生型hFFA2、hFFA3和小鼠FFA2无活性。MOMBA能够在表达hFFA2-DREADD受体的细胞中抑制forskolin刺激的cAMP水平，其功效改善且与山梨酸的效力相当。在hFFA2-DREADD转基因小鼠中，MOMBA治疗显著降低肠道传输速度，并促进依赖浓度的结肠隐窝GLP-1释放。该化合物具有口服生物利用度。

化合物

Cat.No: T8642

Target: GPR

3-chloro-5-hydroxybenzoic Acid

Cat.No: T7482

Target: GPR

Cat.No: T7796

Target: GPR

Cat.No: T15810

Target: GPR

GPR120 Agonist 2

Cat.No: T4312

Synonym: GPR120 receptor agonist

Target: GPR

Cat.No: T3433

Synonym: TUG 891,TUG891

Target: GPR

GPR40/FFAR1 modulator 1

Cat.No: T11458

Target: GPR

Cat.No: T2351

Synonym: TAK875

Target: GPR

AMG 837 calcium hydrate

Cat.No: TQ0020

Target: GPR

Cat.No: T22027

Synonym: AH 7614

Target: GPR

Cat.No: T7127

Target: Apoptosis, GPR

GPR120 Agonist 3

Cat.No: T15413

Synonym: GPR120-IN-1

Target: GPR

Cat.No: T22967

Synonym: MEDICA 16

Target: GPR, Others, ATP Citrate Lyase

Cat.No: T3171

Synonym: GSK 137647

Target: GPR

Cat.No: T12883

Synonym: PBI-4050,3-戊基苯乙酸,Setogepram

Target: GPR

Cat.No: T1781

Synonym: GW 9508

Target: GPR, Potassium Channel

1-methoxycyclopropanecarboxylic acid

Cat.No: T9437

Target: GPR

Cat.No: T34967

Synonym: TUG469,TUG 469

Target: GPR

Cat.No: T17177

Synonym: TUG424

Target: Others

Cat.No: T60184

Target: GPR, PPAR

Spexin acetate(1370290-58-6 free base)

Cat.No: TP1930L1

Target: Neuropeptide Y Receptor

GPR40 agonist 4

Cat.No: T15267

Target: Others

Cat.No: T25508

Synonym: HUHS 2002,HUHS-2002

Cat.No: TQ0241

Target: GPR

Cat.No: T34968

Cat.No: T11583

Target: Others

Cat.No: T26935

Synonym: C-108297,C 108297

Cat.No: T36634

E-3030 free acid

Cat.No: T27228

Synonym: E-3030,E3030,E 3030

GPR40 agonist 6

Cat.No: T61055

Arachidonic Acid-biotin

Cat.No: T38070

Cat.No: T71663

Cat.No: T69824

Cat.No: T70468

Cat.No: T69953

Palmitic acid-13C

Cat.No: T35791

Cat.No: T37896

Cat.No: T35816

Cat.No: T83955

Cat. No.	Product Name	Target	Signaling Pathways
T3919	Ginsenoside Rb2 Ginsenoside C,人参皂苷 Rb2,人参皂苷Rb2	GPR; Others; Influenza Virus; Endogenous Metabolite	Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Others
	Ginsenoside Rb2 (Ginsenoside C) 是人参提取物中的一种主要生物活性成分，具有抗病毒活性，可上调 GPR120 基因表达。
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。
T2P2919	(2S,3R,4S)-4-Hydroxyisoleucine (4S)-4-Hydroxy-L-isoleucine,(4S)4-羟基异亮氨酸,Hydroxyisoleucine	PI3K	PI3K/Akt/mTOR signaling
	(2S,3R,4S)-4-Hydroxyisoleucine (Hydroxyisoleucine) 是分离自胡芦巴中的一种可口服的有效成分，具有抗糖尿病、抗糖尿病肾病的作用。

天然产物

Ginsenoside Rb2

Cat.No: T3919

Synonym: Ginsenoside C,人参皂苷 Rb2,人参皂苷Rb2

Target: GPR, Others, Influenza Virus, Endogenous Metabolite

Cat.No: T1286

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

Target: GPR, Others

(2S,3R,4S)-4-Hydroxyisoleucine

Cat.No: T2P2919

Synonym: (4S)-4-Hydroxy-L-isoleucine,(4S)4-羟基异亮氨酸,Hydroxyisoleucine

Target: PI3K

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