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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
	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
	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
	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。
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。
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。
T69860	PSB-15160
	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
	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
	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
	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
	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

GPR84 antagonist 2

Cat.No: T72536

GPR84 antagonist 1

Cat.No: T62261

Cat.No: T12883

Synonym: PBI-4050,3-戊基苯乙酸,Setogepram

Target: GPR

Cat.No: T2036

Synonym: GTPL5846

Target: GPR

Cat.No: T11411

Target: GPR, Others

Fezagepras sodium

Cat.No: T12375

Synonym: Setogepram sodium salt,PBI-4050 sodium salt

Target: GPR

Cat.No: T69860

Cat.No: T68805

Cat.No: T69824

Cat.No: T37907

Cat.No: T36634

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