GPR84(G蛋白偶联受体84)

GPR84 is a G protein-coupled receptor for medium-chain fatty acids. GPR84 is a receptor for free fatty acids and can be potently activated by saturated medium-chain free fatty acids (MCFAs) like decanoic acid, undecanoic acid and lauric acid. GPR84, a receptor for medium-length free fatty acids is upregulated on protein level in LPS activated tolerant CD14⁺ monocytes and THP-1 cells.

GPR84 is activated by MCFAs with the hydroxyl group at the 2- or 3-position more effectively than nonhydroxylated MCFAs. GPR84 is now considered to be a member of FFA-sensing GPCRs. MCFAs with carbon chain lengths of 9–14 activate GPR84, coupling primarily to a pertussis toxin (PTX)-sensitive G_i/o pathway. GPR84 should be a proinflammatory receptor and may be a novel, attractive target for treating chronic low grade inflammation associated-diseases.

Products for GPR84

Cat.No. 产品名称 Information
GC71501 TUG-2208 TUG-2208(化合物42a)是一种GPR84激动剂(pEC50=8.98)，具有低亲脂性、良好的溶解度、体外渗透性和微粒体稳定性。
GC71478 OX04528 OX04528（化合物68）是一种强效的、G蛋白偏向的、口服活性的GPR84激动剂。
GC69187 GPR84 antagonist 2 GPR84 antagonist 2 (compound 33) 是一种口服有效的，选择性的 GPR84 拮抗剂(IC50=8.95 nM)。GPR84 antagonist 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。GPR84 antagonist 2 具有研究溃疡性结肠炎的潜力。
GC64229 GPR84 antagonist 1 GPR84 antagonist 1 是一种高亲和力、高选择性的人 GPR84 竞争性拮抗剂。
GC31712 GPR84 antagonist 8 GPR84antagonist8是一种选择性GPR84拮抗剂。
GC31698 PBI-4050 sodium salt (Setogepram (sodium salt))
Setogepram sodium; PBI-4050 sodium
Fezagepras (Setogepram) sodium 作为 GPR40 的口服活性激动剂和 GPR84 的拮抗剂或反向激动剂。
GC11350 6-OAU
GTPL5846
An agonist for GPR84