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Search Results for " gpr84 "

Targets Recommended: GPR

14

抑制剂 & 化合物

1

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T11462	GPR84 antagonist 8	GPR	Endocrinology/Hormones; GPCR/G Protein
	GPR84 antagonist 8 is a selective GPR84 antagonist.
T62918	GPR84 antagonist 3	Others	Others
	GPR84antagonist 3 (compound 42)为一种高效GPR84(G 蛋白偶联受体 84)拮抗剂，具pIC50值为8.28，表现出对GTPγS的抑制作用，并拥有良好的药代动力学特性。
T72536	GPR84 antagonist 2	Others	Others
	GPR84antagonist 2 是一种口服有效的，选择性的 GPR84拮抗剂(IC50=8.95 nM)。GPR84antagonist 2 在钙动员试验中显示出更强的效力，并在 GPR84激活时抑制中性粒细胞和巨噬细胞的趋化性。GPR84antagonist 2 具有研究溃疡性结肠炎的潜力。
T62261	GPR84 antagonist 1	Others	Others
	GPR84 antagonist 1 是一种强选择性的、高亲和力的人 GPR84 竞争性拮抗剂。
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。
T2036	6-OAU GTPL5846	GPR	Endocrinology/Hormones; GPCR/G Protein
	6-OAU (GTPL5846) 是 GPR84 的替代激动剂，在 Gqi5 嵌合体存在的情况下，在 HEK293 细胞中激活人 GPR84，在 PI 测定中 EC50 为 105 nM。
T84313	OX04528	cAMP; GPR	Endocrinology/Hormones; GPCR/G Protein
	OX04528 是一种具有口服活性和高效性的 GPR84 偏向激动剂。OX04528 抑制 cAMP 信号传导，可用于研究癌症。
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。
T11411	GLPG1205	GPR; Others	Endocrinology/Hormones; GPCR/G Protein; Others
	GLPG1205是一种有效的、具有口服活性的 GPR84（G 蛋白偶联受体）拮抗剂，具有抗炎活性。GLPG1205显示出良好的PK/PD 特征，可用于研究肺纤维化。
T69860	PSB-15160	Others	Others
	PSB-15160是治疗雌激素依赖性肿瘤的化合物，对MCF7(乳腺)、NCI-H460(肺)和SF-268 (NCS)细胞的生长具有抑制作用。
T68805	PSB-1584	Others	Others
	PSB-1584 is a Potent Agonist of the Orphan G Protein-Coupled Receptor 84 (GPR84). 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.
T69824	PSB-17365	Others	Others
	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.
T37907	DL 175	Others	Others
	Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.
T36634	ZQ 16	Others	Others
	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...

化合物

GPR84 antagonist 8

Cat.No: T11462

Target: GPR

GPR84 antagonist 3

Cat.No: T62918

Target: Others

GPR84 antagonist 2

Cat.No: T72536

Target: Others

GPR84 antagonist 1

Cat.No: T62261

Target: Others

Cat.No: T12883

Synonym: PBI-4050,3-戊基苯乙酸,Setogepram

Target: GPR

Cat.No: T2036

Synonym: GTPL5846

Target: GPR

Cat.No: T84313

Target: cAMP, GPR

Fezagepras sodium

Cat.No: T12375

Synonym: Setogepram sodium salt,PBI-4050 sodium salt

Target: GPR

Cat.No: T11411

Target: GPR, Others

Cat.No: T69860

Target: Others

Cat.No: T68805

Target: Others

Cat.No: T69824

Target: Others

Cat.No: T37907

Target: Others

Cat.No: T36634

Target: Others

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPH-01410	GPR84 Protein, Human, Recombinant (hFc) G-protein coupled receptor 84,GPR84	Human	P. pastoris (Yeast)
	Receptor for medium-chain free fatty acid (FFA) with carbon chain lengths of C9 to C14. Capric acid (C10:0), undecanoic acid (C11:0) and lauric acid (C12:0) are the most potent agonists. Not activated by short-chain and long-chain saturated and unsaturated FFAs. Activation by medium-chain free fatty acid is coupled to a pertussis toxin sensitive G(i/o) protein pathway. May have important roles in processes from fatty acid metabolism to regulation of the immune system. GPR84 Protein, Human, Recom...

重组蛋白

GPR84 Protein, Human, Recombinant (hFc)

Cat.No: TMPH-01410

Species: Human

Expression System: P. pastoris (Yeast)

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