AM679

图片 1

“目录号: HY-14163

我從床鋪上起身
周圍散亂著線圈
塞滿垃圾的圓桶
隨地丟棄的空瓶
濕漉漉的水泥地
折射彩虹的鮮艷
蓬頭垢面的樣貌
昏昏欲睡的面容
空洞呆滯的眼神
索然無趣的興致
渾渾噩噩的晝夜
萎靡不振的日常

12国记完

“目录号: HY-14460 ee.: 99.20%

关注 3012674

Immunology/Inflammation-

泰麒是我最喜欢的,但是没有讲完。。。漂亮的黑麒。。。我总觉得这里面的麒麟模样分明是独角兽。。。这让我想起哈利波特了

Immunology/Inflammation-

献吻 0

AM 103 是具有选择性的,有效的FLAP抑制剂,IC50值为 4.2 nM。

AM679是高活性FLAP抑制剂,对FLAP结合/hLA/hWB的IC50分别为2.2 nM/0.6 nM/154
nM。

献花 0

FLAP

FLAP

2AM

相关产品

相关产品

英文名:

MK-886-MK591-GSK2190915-AM679-MK-0591-

MK-886-MK591-GSK2190915-MK-0591-AM
103-

2AM

生物活性

生物活性

性别:

Description

Description

民族:

AM 103 is a potent and selectiveFLAPinhibitor, with anIC50value
of 4.2 nM.

AM679 is a potent and selective FLAP inhibitor with IC50s of  2.2 nM/0.6
nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6
nM/154 nM(FLAP binding/hLA/hWB) [1]Target: FLAPin vitro: AM679 showed
excellent in vitro inhibition against FLAP. AM679 has an excellent hWB
IC50 potency of 154 nM. AM679 showed an improved CYP inhibition profile
(IC50 3A4 = 16.7 lM, 2C9 = 3.7 lM, 2D6 >30 lM), no time dependent
inhibition against CYP3A4 (0.003 min-1 vs 0.057 min-1 for troleandomycin
control  10 uM) and no CYP3A4 induction.in vivo: AM679 was profiled in a
rodent bronchoalveolar lavage (BAL) model to measure its ability to
inhibit production ofleukotrienes in vivo.16 Oral administration of 39
(10 mg/kg as the sodium carboxylate salt) 4 h prior to ionophore
challenge reduced LTB4 and CysLT levels in the rodent lung lavage fluid
by 98% and 87%, respectively, with corresponding average rodent plasma
levels of 605 nM (3 h post dose, rat blood LTB4 IC50 = 125 nM).

朝鲜族

IC50& Target

References

身高:

IC50: 4.2 nM
(FLAP)[1];)

[1].Stock, N, et al. 5-Lipoxygenase-activating protein inhibitors.
Part 2:
3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic
acid (AM679)-A potent FLAP
inhib

生日:

In Vitro

[2].Musiyenko, A, et al. A novel 5-lipoxygenase-activating protein
inhibitor, AM679, reduces inflammation in the respiratory syncytial
virus-infected mouse eye. Clinical and Vaccine Immunology (2009),
16(11),
1654-1659.

体重:

AM 103 has an IC50value of 349 nM in the human blood LTB4 inhibition
assay. AM 103 has an excellent CYP profile against the 5 most common CYP
isoforms with IC50values greater than 30 μM for CYP2D6 and >50 μM for
CYPs 3A4, 2C9 2C19, and
1A2[1];).
AM103 is a novel, potent, and selective FLAP inhibitor with IC50values
of 350, 113, and 117 nM against human, rat, and mouse whole-blood
ionophore-stimulated LTB4 production,
respectively[2];).

生肖:

In Vivo

国籍:

AM 103 has high bioavailability (64%), low clearance (2.9 mL/min/kg),
low volume of distribution (0.41 L/kg), and a long i.v. half-life (5.2
h) in dogs. AM 103 (10 mg/kg q.i.d.) inhibits the increase in CysLTs and
EPO by approximately 60%, and IL-5 levels are reduced to the
concentrations obtained following saline treatment alone in
mice[1];).
AM103 (1 mg/kg, p.o.) displays >50% inhibition for up to 6 h with a
calculated EC50of appr 60 nM, in a rat ex vivo whole-blood calcium
ionophore-induced LTB4 assay. AM 103 inhibits LTB4 and cysteinyl
leukotriene (CysLT) production with ED50values of 0.8 and 1 mg/kg,
respectively, when rat lung is challenged in vivo with calcium
ionophore. In this model, the EC50derived from plasma AM103 is appr 330
nM for inhibition of both LTB4 and CysLT. In a model of chronic lung
inflammation using ovalbumin-primed and challenged BALB/c mice, AM103
reduces the concentrations of eosinophil peroxidase, CysLTs, and
interleukin-5 in the bronchoalveolar lavage fluid. Finally, AM 103
increases survival time in mice exposed to a lethal intravenous
injection of platelet-activating
factor[2];).

韩国

References

星座:

[1].Hutchinson JH, et al. 5-lipoxygenase-activating protein
inhibitors: development of
3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic
acid (AM103). J Med Chem. 2009 Oct
8;52(19):5803-15.

出生地:

[2].Lorrain DS, et al. Pharmacological characterization of
3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic
acid (AM103), a novel selective 5-lipoxygenase-activating protein
inhibitor that reduces acute and chronic inflammation. J Pharmacol Exp
Ther. 2009
Dec;331(3):1042-50.

血型:

职 业:

毕业院校:

所属公司:

代表作品:

《这首歌》《不接电话的你》《死也不能放开你》《某个春日》

2AM,韩国JYP Entertainment公司于2008年推出的四人男子组合(同属Big Hit
Entertainment,BigHitE.负责经营管理),四名成员分别是从团队综艺选拔出的赵权(队长),任瑟雍,郑珍云,以及后来加入的李昶旻。四人以在舞台上的沉稳以及接近于完美的演唱能力被歌迷所熟知,音乐风格如同名称一般,在凌晨两点的深夜里,能感受到最宁静的时刻。是韩国组合里唱功最好的团体之一。

主要成就

1、08Asia Song Festival亚洲新人赏

2、08文化体育观光部 优秀新人专辑

3、10亚洲音乐盛典 最佳演唱团体奖

4、韩国金唱片大赏 音源大赏、本赏

5、声音海洋Soribada最佳男子团体奖

6、Melon Music Awards十大歌手奖

7、Melon Music Awards年度最佳歌曲

8、10大韩民国国会大赏 大众音乐奖

9、首尔歌谣大赏 R&B抒情部门赏

10、首尔歌谣大赏 本赏

星路历程

音乐

《One day》
《Fitzgerald式的爱情故事》
《只要好好吃饭》
《告白的日子》
《唠叨》
《我错了》
《死也不能放开你》
《我们相爱了》
《不要强忍》
《毕业》
《这首歌》

发表评论

电子邮件地址不会被公开。 必填项已用*标注