GTPL5846

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

6-OAU(GTPL5846; 6-n-辛基氨基尿嘧啶) 是 GPR84 的替代激动剂；在 HEK293 细胞中存在 Gqi5 嵌合体的情况下激活人 GPR84，在 PI 测定中 EC50 为 105 nM。

6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

GPR84 gene exhibits high expression in human polymorphonuclear leukocytes (PMNs) and macrophages, 6-OAU acts on proinflammatory function by activitating GPR84.6-OAU (0.01 nM-0.1 mM; 1 h) activates human GPR84 in the presence of Gqi5 chimera with an EC50 value of 105 nM in HEK293 cells.6-OAU (0, 6.25, 200 μM; 30 min) stimulates [35S]GTP binding, accumulates phosphoinositides, and induces GPR84-EGFP internalization in a GPR84-dependent manner.6-OAU (1 nM-1 mM; 1 h) provokes chemotaxis of PMNs in a concentration-dependent manner with an EC50 value of 318 nM.6-OAU (0-10 μM; 4 h) increases the secretion of IL-8 from LPS-stimulated PMNs.6-OAU (0-0.4 μM; 16 h) also amplifies TNF-α production from U937 macrophages.6-OAU (2 μM; 4 h) decreases ERK phosphorylation and MCP-1 protein expression, (2 μM; 48 h) decreases MCP-1 secretion in macrophages .6-OAU (2 μM; 24 h) reduces ROS production during B. abortus infection in RAW264.7 cells.6-OAU (2 μM; 0, 30, and 60 min) inhibits adhesion and Brucella uptake in RAW264.7 cells and (2 μM; 30 min) shows anti-infection against Brucella and Salmonella infection.Cell Viability Assay Cell Line:B. abortus Concentration:0, 0.02, 0.2, 2 μM Incubation Time:0, 2, 24, 48, 72 hours Result:Decreased B. abortus survivability begin at 48 h with a dose of 2 μM.Western Blot Analysis Cell Line:RAW264.7 cells infected with B. abortus Concentration:2 μM Incubation Time:4 hours Result:Reduced ERK phosphorylation and MALT1 expression in RAW264.7 macrophages.

6-OAU activates GPR84 and results in making an inflammatory condition through chemokine production and chemotaxis in vivo.6-OAU (10 mg/kg; i.v.) raises the blood CXCL1 level in rats.6-OAU (1 mg/mL; s.c.) attracts both PMNs and macrophages into the air pouch.6-OAU (2 μM, 100 mL/mouse; s.c.) augments resistance to Brucella infection, and reduces bacterial proliferation in spleens and livers. Animal Model:Female Lewis rats(4-week-old) Dosage:10 mg/kg Administration:Intravenous injection; collecting blood 3 h after injection Result:Increased the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection.Animal Model:Rat air pouch model (4-week-old female rats)Dosage:1 mg/mL (PBS) Administration:Subcutaneous injection; washing the cavity 4 h after injection Result:Attracted both PMNs and macrophages into the air pouch, peaking at 4 h after the injection.Animal Model:ICR female mice (7-week-old) Dosage:2 μM (100 μL/mouse) Administration:Oral average; 7 days and another 14 days after treated mouse with B. abortus (2 × 105 CFU /100 μL; i.p.)Result:Reduced bacterial proliferation in the liver and spleen, and decreased IFN-γ but augmented IL-6 serum level.

GTPL5846 | GTPL 5846 | GTPL-5846.

Cell Cycle/DNA Damage

GPR

GPR84

Inflammation/Immunology

——

83797-69-7

239.31

C12H21N3O2

>98% (HPLC)

DMSO: 10 mM

O=C1NC(C=C(NCCCCCCCC)N1)=O

6-(Octylamino)-2,4(1H,3H)-pyrimidinedione

(-20℃)

With Ice Pack

≥ 2 years