1. GPCR/G Protein Stem Cell/Wnt MAPK/ERK Pathway Anti-infection
  2. GPR84 ERK Bacterial Antibiotic
  3. 6-OAU

6-OAU  (Synonyms: GTPL5846)

目录号: HY-12764 纯度: 99.91%
COA 产品使用指南

6-OAU (GTPL5846) 是一种 GPR84 (G 蛋白偶联受体 84) 激动剂,EC50 为 105 nM。6-OAU 对中性粒细胞和巨噬细胞都有趋化作用,并扩增促炎细胞因子 IL-8,表现出促炎功能。6-OAU 还具有抗细菌感染能力。

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6-OAU Chemical Structure

6-OAU Chemical Structure

CAS No. : 83797-69-7

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10 mM * 1 mL in DMSO ¥3190
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC50 value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function[1][2].

IC50 & Target

ERK

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.0167 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
[PMID: 31721581]
CHO EC50
0.114 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
[PMID: 31721581]
HEK293 EC50
0.105 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
[PMID: 31721581]
HEK293 EC50
0.341 μM
Compound: 3
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF as
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF as
[PMID: 31721581]
HEK293 EC50
0.653 μM
Compound: 6-OAU
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
[PMID: 27326330]
HEK293 EC50
1.25 μM
Compound: 3
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
[PMID: 31721581]
HEK293 EC50
1.75 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
[PMID: 31721581]
HEK293 EC50
438 nM
Compound: 6-OAU
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
[PMID: 27326330]
Sf9 EC50
0.512 μM
Compound: 3
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
[PMID: 31721581]
Sf9 EC50
512 nM
Compound: 6-OAU
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
[PMID: 27326330]
体外研究
(In Vitro)

GPR84 gene exhibits high expression in human polymorphonuclear leukocytes (PMNs) and macrophages, 6-OAU acts on proinflammatory function by activitating GPR84[1].
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[1].
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[1].
6-OAU (1 nM-1 mM; 1 h) provokes chemotaxis of PMNs in a concentration-dependent manner with an EC50 value of 318 nM[1].
6-OAU (0-10 μM; 4 h) increases the secretion of IL-8 from LPS-stimulated PMNs[1].
6-OAU (0-0.4 μM; 16 h) also amplifies TNF-α production from U937 macrophages[1].
6-OAU (2 μM; 4 h) decreases ERK phosphorylation and MCP-1 protein expression, (2 μM; 48 h) decreases MCP-1 secretion in macrophages [2].
6-OAU (2 μM; 24 h) reduces ROS production during B. abortus infection in RAW264.7 cells[2].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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[2]

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.
体内研究
(In Vivo)

6-OAU activates GPR84 and results in making an inflammatory condition through chemokine production and chemotaxis in vivo[1].
6-OAU (10 mg/kg; i.v.) raises the blood CXCL1 level in rats[1].
6-OAU (1 mg/mL; s.c.) attracts both PMNs and macrophages into the air pouch[1].
6-OAU (2 μM, 100 mL/mouse; s.c.) augments resistance to Brucella infection, and reduces bacterial proliferation in spleens and livers[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats(4-week-old)[1]
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)[1]
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)[2]
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.
Lowed splenic weight of mice and splenic proliferation.
分子量

239.31

Formula

C12H21N3O2

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 25 mg/mL (104.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1787 mL 20.8934 mL 41.7868 mL
5 mM 0.8357 mL 4.1787 mL 8.3574 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.91%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.1787 mL 20.8934 mL 41.7868 mL 104.4670 mL
5 mM 0.8357 mL 4.1787 mL 8.3574 mL 20.8934 mL
10 mM 0.4179 mL 2.0893 mL 4.1787 mL 10.4467 mL
15 mM 0.2786 mL 1.3929 mL 2.7858 mL 6.9645 mL
20 mM 0.2089 mL 1.0447 mL 2.0893 mL 5.2234 mL
25 mM 0.1671 mL 0.8357 mL 1.6715 mL 4.1787 mL
30 mM 0.1393 mL 0.6964 mL 1.3929 mL 3.4822 mL
40 mM 0.1045 mL 0.5223 mL 1.0447 mL 2.6117 mL
50 mM 0.0836 mL 0.4179 mL 0.8357 mL 2.0893 mL
60 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7411 mL
80 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3058 mL
100 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0447 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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6-OAU
目录号:
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